Compounds having activity against potyvirus and methods of making and using the same

By introducing Boc-glycylproline into the cytosine nucleoside structure, a new compound was designed and synthesized, which solved the problem of low activity of existing drugs against Potato Virus Y, and achieved highly efficient prevention and control of Potato Virus Y, with broad application prospects.

CN116574146BActive Publication Date: 2026-05-29SHENYANG AGRI UNIV

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHENYANG AGRI UNIV
Filing Date
2023-05-18
Publication Date
2026-05-29

AI Technical Summary

Technical Problem

Existing drugs have low antiviral activity against the potato virus Y genus and cannot meet production needs, so there is an urgent need to develop new and highly effective antiviral agents.

Method used

A new compound was designed and synthesized by introducing Boc-glycylproline into the cytosine nucleoside lead structure, and prepared through a specific synthetic route for the prevention and control of Potato Virus Y.

Benefits of technology

This compound exhibits significant preventive and therapeutic activity against potato virus Y, sugarcane mosaic virus, and turnip mosaic virus, outperforming commercially available pesticides, and is widely used in the preparation of antiviral pesticides for plants.

✦ Generated by Eureka AI based on patent content.

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Abstract

The application belongs to the field of agricultural chemicals, and particularly relates to a compound with anti-potato virus Y virus activity and a preparation method and application thereof. 16 H 23 N5O7, the compound provided by the application has good inhibiting effect on viruses of the potato virus Y, such as potato virus Y, sugarcane mosaic virus and turnip mosaic virus, and can be used for preparation of anti-plant virus pesticides, and has wide application prospect.
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Description

Technical Field

[0001] This invention belongs to the field of agricultural chemicals, specifically relating to compounds with activity against Potato Virus Y, their preparation methods, and applications. Background Technology

[0002] Potato virus Y (PVY) has a wide host range, infecting plants in the Solanaceae, Amaranthaceae, Chenopodiaceae, Asteraceae, and Fabaceae families. Mechanical inoculation can infect up to 120 plant species. This genus is the largest of the plant virus genus, and many of its viruses are important pathogens that harm food crops, cash crops, forage grasses, medicinal herbs, and fruit trees, causing serious economic losses worldwide.

[0003] Pyrimidine nucleosides are commonly used in the pesticide field as fungicides or antiviral agents. Among them, pyrimidine nucleoside antibiotics (such as agricultural antibiotic 120) are widely used microbial pesticides, effective against fungal diseases such as wilt, root rot, and damping-off, as well as bacterial diseases such as bacterial angular leaf spot, soft rot, black rot, bacterial wilt, and crown gall. Commercially available drugs such as ningnanmycin, yunnanmycin, and ribavirin are all pyrimidine nucleoside drugs with antiviral and fungicidal effects. However, existing drugs have low antiviral activity against Potato Virus Y, which cannot meet production needs; therefore, there is an urgent need to develop new antiviral agents. Summary of the Invention

[0004] This invention utilizes the principles of pesticide molecular design to introduce Boc-glycylproline into the cytosine nucleoside lead structure, thereby designing and synthesizing a compound that is highly effective against potato virus Y. Systematic bioactivity screening was conducted, providing new and highly efficient candidate compounds for the creation of novel pesticides.

[0005] In a first aspect, the present invention provides a compound having activity against Potato Virus Y, having the structural formula shown in Formula IV below:

[0006]

[0007] A second aspect of the present invention provides a method for preparing the compound, wherein the synthetic route is as follows:

[0008]

[0009] Among them, compound I is Boc-glycylproline, and compound II is cytosine nucleoside.

[0010] Furthermore, the specific operations of each step in the preparation method are as follows:

[0011] 1) Preparation of compound III:

[0012] Boc-glycylproline and cytosine nucleoside were mixed, and N,N-dimethylformamide was added as a solvent. A condensing agent was then added, and the mixture was stirred at room temperature for 4–16 hours. The reaction mixture was purified by ACN / H2O through a pentafluorophenyl column to obtain compound III.

[0013] 2) Preparation of compound IV:

[0014] Compound III, tetrahydrofuran, and trifluoroacetic acid were mixed and stirred at room temperature for 1–2 hours. After the reaction was completed, the product was separated by thin-layer chromatography and then concentrated. The concentrated product was purified by ACN / H2O through a pentafluorophenyl column to obtain compound IV.

[0015] Furthermore, in step 1), the condensing agent is 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and N,N-diisopropylethylamine.

[0016] Furthermore, in step 1), the mass-to-volume ratio of Boc-glycylproline, cytosine nucleoside, N,N-dimethylformamide, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and N,N-diisopropylethylamine is 4-15g:4-20g:5-12ml:3-9g:4-15g.

[0017] Furthermore, in step 1), the volume ratio of ACN / H2O is 1 to 4 / 1 to 8.

[0018] Furthermore, in step 2), the mass-to-volume ratio of compound III, tetrahydrofuran, and trifluoroacetic acid is 4–16 g: 5–9 ml: 1–5.

[0019] Furthermore, in step 2), thin-layer chromatography uses ethyl acetate / petroleum ether at a volume ratio of 1-2:2-3 as the chromatography solvent, quenches the reaction with saturated sodium bicarbonate solution, and extracts with ethyl acetate to separate the ethyl acetate layer. The ethyl acetate phase is then washed successively with water and saturated sodium chloride, separated and concentrated under vacuum to obtain the concentrated product.

[0020] Furthermore, in step 2), the volume ratio of ACN / H2O is 1 to 3 / 4 to 7.

[0021] A third aspect of the invention provides the use of the compound in the preparation of agents for the prevention and control of plant viruses, including potato virus Y, sugarcane mosaic virus and turnip mosaic virus.

[0022] Compared with the prior art, the present invention has the following beneficial effects:

[0023] The compound provided by this invention, which exhibits activity against Potato Virus Y (PVY), is a novel compound with antiviral activity against plant viruses. The preparation method of this compound has advantages such as readily available raw materials, mild reaction conditions, and simple operation. The compound demonstrates significantly higher preventive and curative activity against Potato Virus Y (PVY), Sugarcane Mosaic Virus (SCMV), and Turnip Mosaic Virus (TuMV) than commercially available pesticides, and can be used in the preparation of antiviral pesticides, showing broad application prospects. Attached Figure Description

[0024] Figure 1 This is the structural formula of compound IV.

[0025] Figure 2 This is the synthetic route for compound IV. Detailed Implementation

[0026] The present invention will now be described in detail with reference to the accompanying drawings and specific embodiments, but this should not be construed as limiting the invention. Unless otherwise specified, the technical means used in the following embodiments are conventional means well known to those skilled in the art, and the materials, reagents, etc. used in the following embodiments are commercially available unless otherwise specified.

[0027] Example 1: Preparation of Compound IV

[0028] like Figure 2 The synthetic route shown involves adding 4g of compound I (Boc-glycylproline) and 4g of compound II (cytosine nucleoside) to a 50ml round-bottom flask, evacuating the flask, and then adding 5ml of dry N,N-dimethylformamide (DMF) as a solvent. Next, 3g of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDCI) and 4g of N,N-diisopropylethylamine (DIEA) are added as condensing agents. The mixture is stirred at room temperature for 4 hours. The reaction mixture is purified by pentafluorophenyl column chromatography using ACN / H2O (v / v = 1 / 5) to give compound III, namely tert-butyl(2-(2-((1-(3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)carbamoyl)pyrrolidine-1-yl)-2-carbonylethyl)carbamate. The amount of compound III prepared and the volume of the reaction vessel are increased or decreased proportionally.

[0029] 4 g of compound III tert-butyl(2-(2-(((1-(3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)carbamoyl)pyrrolidine-1-yl)-2-carbonylethyl)carbamate was added to a 50 mL round-bottom flask, and the mixture was evacuated. 5 mL of tetrahydrofuran (THF) and 1–5 mL of trifluoroacetic acid (TFA) were added. The mixture was stirred at room temperature for 1 hour. The reaction was monitored by silica gel thin-layer chromatography using ethyl acetate:petroleum ether = 1:3 as the chromatographic solvent. The reaction was quenched with saturated sodium bicarbonate solution, and the ethyl acetate layer was extracted with ethyl acetate. The ethyl acetate phase was washed successively with water and saturated sodium chloride, and then separated and concentrated under vacuum. The mixture was purified by pentafluorophenyl column chromatography with ACN / H₂O (v / v = 1 / 4), followed by separation and concentration under vacuum to give compound IV, namely N-(1-(3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)-1-glycylpyrrolidine-2-carboxamide. The amount of compound IV prepared and the volume of the reaction vessel were scaled up or down proportionally. The chemical name of compound IV is: (S)-N-(1-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)-1-glycylpyrrolidine-2-carboxamide, and its chemical formula is: C 16 H 23 The physicochemical and structural parameters of N5O7 and compound IV are shown in Table 1.

[0030] Table 1 Physicochemical and structural parameters of compound IV

[0031]

[0032] Example 2 Preparation of Compound IV

[0033] like Figure 2The synthetic route shown involves adding 15 g of compound I (Boc-glycylproline) and 15 g of compound II (cytosine nucleoside) to a 50 ml round-bottom flask, evacuating the flask, and then adding 5–12 ml of dry N,N-dimethylformamide (DMF) as a solvent. Next, 8 g of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDCI) and 6 g of N,N-diisopropylethylamine (DIEA) are added as condensing agents. The mixture is stirred at room temperature for 16 hours. The reaction mixture is purified by pentafluorophenyl column chromatography using ACN / H₂O (v / v = 4 / 1) to give compound III, namely tert-butyl(2-(2-((1-(3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)carbamoyl)pyrrolidine-1-yl)-2-carbonylethyl)carbamate. The amount of compound III prepared and the volume of the reaction vessel are increased or decreased proportionally.

[0034] 12 g of compound III tert-butyl(2-(2-(((1-(3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)carbamoyl)pyrrolidine-1-yl)-2-carbonylethyl)carbamate was added to a 50 mL round-bottom flask, and the mixture was evacuated. 9 mL of tetrahydrofuran (THF) and 5 mL of trifluoroacetic acid (TFA) were added. The mixture was stirred at room temperature for 2 hours. The reaction was monitored by silica gel thin-layer chromatography using ethyl acetate:petroleum ether = 2:3 as the chromatographic solvent. The reaction was quenched with saturated sodium bicarbonate solution, and the ethyl acetate layer was extracted with ethyl acetate. The ethyl acetate phase was washed successively with water and saturated sodium chloride, and then separated and concentrated under vacuum. The mixture was purified by pentafluorophenyl column chromatography using ACN / H₂O (v / v = 1 / 4), followed by separation and concentration under vacuum to obtain compound IV, namely N-(1-(3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)-1-glycylpyrrolidine-2-carboxamide. The amount of compound IV prepared and the volume of the reaction vessel were scaled up or down proportionally. The physicochemical and structural parameters of the compound are shown in Table 1.

[0035] Example 3: Activity assay against potato virus Y in tobacco crops

[0036] Potato virus Y (PVY) damage on tobacco is severe and widespread, causing significant losses. This invention uses a disease index method to determine the activity of compound IV against PVY on tobacco. The specific steps are as follows: Compound IV, prepared in Example 1, is diluted to a test solution with a mass concentration of 100 mg / L. Ningnanmycin and copper morpholine guanidine technical grade at the same concentration are used as controls, and Tween 80 aqueous solution is used as a blank control. Common tobacco plants with uniform growth at the 5-6 leaf stage are selected. The agent is evenly sprayed onto the leaf surface of the test host. 24 hours after spraying, PVY virus is inoculated (preventive activity). 24 hours after PVY inoculation, the agent is sprayed again (therapeutic activity). Fresh virus-infected leaves are taken and homogenized with PBS buffer (pH = 7.2). Carborundum (240 mesh) is sprayed onto the leaves. The 3rd and 4th leaves of each common tobacco plant are inoculated using a friction inoculation method. 15 minutes after inoculation, the carborundum is rinsed off the leaf surface with water. Plant symptoms were observed and recorded 21 days after virus inoculation, and the inhibition rate was calculated using the disease index method. Both the treatment and the control were performed in triplicate.

[0037] Grading Standards for Tobacco Virus Diseases (GB / T 23222-2008): Grade 0: No disease in the whole plant; Grade 1: Clear veins in the central leaves or slight mosaic, no obvious stunting of the plant; Grade 3: 1 / 3 of the leaves are mosaic but not deformed, or the plant is stunted to more than 3 / 4 of the normal height; Grade 5: 1 / 3 to 1 / 2 of the leaves are mosaic, or a few leaves are deformed, or the main vein turns black, or the plant is stunted to 2 / 3 to 3 / 4 of the normal height; Grade 7: 1 / 2 to 2 / 3 of the leaves are mosaic or deformed, or the main and lateral veins are necrotic, and the plant is stunted to 1 / 2 to 2 / 3 of the normal height; Grade 9: All leaves of the plant are mosaic, severely deformed or necrotic, and the plant is stunted to more than 1 / 2 of the normal height.

[0038] Disease index = ∑(Disease grade number × Number of plants at that grade) / (Highest disease grade number × Total number of plants surveyed) × 100

[0039] Prevention and control effect (%) = [(disease index of blank control area - disease index of treatment area) / disease index of blank control area] × 100.

[0040] The antiviral activity of compound IV, a highly effective drug for the prevention and control of potato virus Y, according to calculations is shown in Table 2. The results show that compound IV has good preventive and therapeutic activities against potato virus Y. The preventive activity of compound IV is 78.77%, which is higher than that of the control drugs ningnanmycin and ethacrylamide; the therapeutic activity of compound IV is 65.20%, which is significantly higher than that of the control drugs.

[0041] Table 2 Antiviral activity of compound IV

[0042]

[0043] Example 4: Activity assay against sugarcane mosaic virus on maize crop

[0044] Sugarcane mosaic virus (SCMV) is a major pathogen in maize production in my country and Africa, widely distributed in major maize-producing areas worldwide. Infection of maize alone can cause maize dwarf mosaic disease, leading to yield losses of up to 50%. This invention uses the single-plant leaf damage method to determine the antiviral activity of compound IV against SCMV. The specific steps are as follows: Compound IV prepared in Example 2 is prepared into a test solution with a mass concentration of 100 mg / L. Ningnanmycin and copper morpholine guanidine technical grade at the same concentration are used as controls, and Tween 80 aqueous solution is used as a blank control. Maize plants with uniform growth at the 3-4 leaf stage are selected. After spraying the agent for 24 hours, SCMV is inoculated (preventive activity). The agent is sprayed again 24 hours after SCMV inoculation (curative activity). Fresh virus-infected leaves are taken, the midrib removed, and ground into a homogenate with 0.1 M phosphate buffer (pH=7). Carborundum (600 mesh) is sprayed onto the leaves, and the heart leaves of each maize plant are inoculated using a friction inoculation method. A second inoculation is performed when the plant has 5-6 leaves. The morbidity rate was investigated 21 days after the second inoculation, and the disease index was investigated three weeks after the maize tasseled. Both the treatment and control were repeated three times.

[0045] Grading standards for maize viral diseases: Grade 0: No disease in the whole plant; Grade 1: The maize plant shows chlorotic lines or stripes from the base of the leaves, or 1-2 leaves show slight chlorotic symptoms, with no yield reduction or mild yield reduction; Grade 2: Most of the leaves above the female ear show slight chlorosis or 1-2 leaves show obvious chlorosis, the height of the diseased plant is slightly lower than that of the healthy plant, the ears are slightly smaller, and the yield reduction is mild; Grade 3: Most of the leaves above the female ear show obvious chlorosis or 1-2 leaves show severe chlorosis, the plant height is significantly reduced, and the yield is reduced by 50%; Grade 4: Most of the leaves show obvious chlorosis or some leaves show severe chlorosis, the plant height is reduced by more than 20%, the rate of empty stalks is high, and the yield is severely reduced or close to zero; Grade 5: Most or all of the leaves of the diseased plant show severe chlorosis, the plant height is significantly reduced, sometimes less than half that of the healthy plant, the plant does not tassel or silk, or although it tassels or silks, it does not produce grains, or it dies before tasseling, resulting in zero or near-zero yield.

[0046] Incidence rate (%) = Number of infected plants / Total number of plants surveyed × 100;

[0047] Disease index = ∑(number of diseased plants at each level × disease level value) / total number of plants surveyed × highest level value × 100.

[0048] The antiviral activity of compound IV, a highly effective drug for the prevention and control of potato virus Y, according to calculations are shown in Table 2. The results show that compound IV has good preventive and therapeutic activities against corn sugarcane mosaic virus. The preventive activity of compound IV is 85.48%, which is higher than that of the control drugs ningnanmycin and ethacrylamide; the therapeutic activity of compound IV is 68.56%, which is also higher than that of the control drugs.

[0049] Example 5: Activity determination against turnip mosaic virus on Chinese cabbage crop

[0050] Turnip mosaic virus (TuMV) can infect cruciferous vegetables, as well as spinach, garland chrysanthemum, and mustard greens. This invention uses a disease index method to determine the antiviral activity of compound IV against TuMV. The specific steps are as follows: Compound IV prepared in Example 1 is prepared into a test solution with a mass concentration of 100 mg / L. Ningnanmycin and copper morpholine guanidine technical grade at the same concentration are used as controls, and Tween 80 aqueous solution is used as a blank control. Fresh diseased leaves of Chinese cabbage infected with TuMV are taken, rinsed with tap water, ground into juice using a mortar and pestle, and added to a phosphate buffer solution at pH 7.0, 0.05 mol / L, at a ratio of 1:4. Carborundum (240 mesh) is sprayed onto the surface of the test host (Chinese cabbage) leaves to inoculate the virus through mechanical friction. TuMV is inoculated 24 hours after spraying (preventive activity), and the drug is sprayed 24 hours after TuMV inoculation (therapeutic activity). The disease index is investigated after 21 days, and the relative efficacy is calculated.

[0051] Grading standards for viral diseases in Chinese cabbage: Grade 0: No symptoms. Grade 1: Visible veins in the heart leaves, slight mosaic pattern. Grade 3: Obvious mosaic pattern, mosaic on the heart and middle leaves. Grade 5: Severe mosaic pattern, some leaves wrinkled and deformed, slight stunting of the plant. Grade 7: Severe mosaic pattern, most leaves wrinkled and deformed, slight necrosis of leaf veins, stunted plant. Grade 9: Severe mosaic pattern, wrinkled and deformed leaves, necrosis of leaf veins, plant stops growing or dies.

[0052] Disease index = ∑(Disease grade number × Number of plants at that grade) / (Highest disease grade number × Total number of plants surveyed) × 100

[0053] Prevention and control efficacy (%) = [(Disease index in blank control area - Disease index in treatment area) / Disease index in blank control area] × 100

[0054] The results of the antiviral activity determination of the compound of the present invention for highly effective prevention and control of potato virus Y are shown in Table 2. The results show that compound IV has good preventive and therapeutic activities against turnip mosaic virus on Chinese cabbage. The preventive activity of compound IV is 79.65%, which is better than the control agents ningnanmycin and copper morpholine guanidine; the therapeutic activity of compound IV is 78.7%, which is better than the control agents.

[0055] Example 6: Field efficacy determination of compound IV against potato virus Y in tomato

[0056] Tomato viral diseases are among the most significant diseases affecting tomato production. The main pathogen is Potato Virus Y (PVY), a major disease that is easy to occur and difficult to control in tomato production. Compound IV has shown good efficacy against PVY in laboratory settings. Therefore, a field efficacy trial was conducted to investigate the effect of Compound IV on PVY in tomatoes.

[0057] This invention uses the disease index method to determine the antiviral activity of compound IV against PVY on tomatoes. The specific steps are as follows: Compound IV, prepared in Example 2, is diluted to a test solution with a mass concentration of 100 mg / L. Ningnanmycin and copper morpholine guanidine technical grade at the same concentration are used as controls, and Tween 80 aqueous solution is used as a blank control. Tomatoes at the 4-true-leaf stage in the field are selected, and the agent is evenly sprayed onto the leaf surface of the test host. 24 hours after spraying, the plant is inoculated with PVY virus (preventative activity), and 24 hours after PVY inoculation, the agent is sprayed again (therapeutic activity). Plant symptoms are observed and recorded 21 days after inoculation, and the inhibition rate is calculated using the disease index method. Both the treatment agent and the control are replicated three times.

[0058] Grading standards for tomato viral diseases: Grade 0, no symptoms; Grade 1, only slight mosaic or streaks on the upper leaves; Grade 2, obvious mosaic or streaks on the upper leaves, leaf deformation, and slight stunting of the plant; Grade 3, deformed leaves, many streaks on the stem, twisted stem, and slight stunting of the plant; Grade 4, severely stunted plant, withered upper leaves.

[0059] Disease index = ∑(Disease grade number × Number of plants at that grade) / (Highest disease grade number × Total number of plants surveyed) × 100

[0060] Prevention and control efficacy (%) = [(Disease index in blank control area - Disease index in treatment area) / Disease index in blank control area] × 100

[0061] The field efficacy of compound IV, a highly effective control of potato virus Y, according to calculations is shown in Table 3. The results show that compound IV has good preventive and curative activity against PVY virus disease on tomatoes in the field. The preventive activity of compound IV is 85.28%, which is significantly higher than that of the control agents ningnanmycin and copper morpholine guanidine. The curative activity of compound IV is 66.25%, which is also higher than that of the control agents ningnanmycin and copper morpholine guanidine.

[0062] Table 3 Field efficacy determination of compound IV

[0063]

[0064] It should be noted that when numerical ranges are mentioned in the claims of this invention, it should be understood that the two endpoints of each numerical range and any value between the two endpoints can be selected. To avoid redundancy, the present invention describes preferred embodiments.

[0065] Although preferred embodiments of the invention have been described, those skilled in the art, upon learning the basic inventive concept, can make other changes and modifications to these embodiments. Therefore, the appended claims are intended to be interpreted as including both the preferred embodiments and all changes and modifications falling within the scope of the invention.

[0066] Obviously, those skilled in the art can make various modifications and variations to this invention without departing from its spirit and scope. Therefore, if these modifications and variations fall within the scope of the claims of this invention and their equivalents, this invention also intends to include these modifications and variations.

Claims

1. A compound with activity against Potato Virus Y, characterized in that, The structural formula is shown in equation IV below: 。 2. The method for preparing the compound according to claim 1, characterized in that, The synthetic route is as follows: ; Among them, compound I is Boc-glycylproline, and compound II is cytosine nucleoside.

3. The preparation method according to claim 2, characterized in that, The specific steps are as follows: 1) Preparation of compound III: Boc-glycylproline and cytosine nucleoside were mixed, and N,N-dimethylformamide was added as a solvent. A condensing agent was then added, and the mixture was stirred at room temperature for 4–16 hours. The reaction mixture was purified by ACN / H2O through a pentafluorophenyl column to obtain compound III. The condensing agent was 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and N,N-diisopropylethylamine. 2) Preparation of compound IV: Compound III, tetrahydrofuran, and trifluoroacetic acid were mixed and stirred at room temperature for 1–2 hours. After the reaction was completed, the product was separated by thin-layer chromatography and then concentrated. The concentrated product was purified by ACN / H2O through a pentafluorophenyl column to obtain compound IV.

4. The preparation method according to claim 3, characterized in that, In step 1), the mass-to-volume ratio of Boc-glycylproline, cytosine nucleoside, N,N-dimethylformamide, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and N,N-diisopropylethylamine is 4-15 g: 4-20 g: 5-12 ml: 3-9 g: 4-15 g.

5. The preparation method according to claim 4, characterized in that, In step 1), the volume ratio of ACN / H2O is 1 to 4 / 1 to 8.

6. The preparation method according to claim 5, characterized in that, In step 2), the mass-to-volume ratio of compound III, tetrahydrofuran, and trifluoroacetic acid is 4–16 g: 5–9 ml: 1–5 ml.

7. The preparation method according to claim 6, characterized in that, In step 2), thin-layer chromatography uses ethyl acetate / petroleum ether at a volume ratio of 1-2:2-3 as the chromatography solvent. The reaction is quenched with saturated sodium bicarbonate solution and extracted with ethyl acetate to separate the ethyl acetate layer. The ethyl acetate phase is washed successively with water and saturated sodium chloride, and then separated and concentrated under vacuum to obtain the concentrated product.

8. The preparation method according to claim 7, characterized in that, In step 2), the volume ratio of ACN / H2O is 1 to 3 / 4 to 7.

9. The use of the compound of claim 1 in the preparation of an agent for the prevention and control of plant viruses, characterized in that, The plant viruses include potato virus Y, sugarcane mosaic virus, and turnip mosaic virus.