Method for synthesizing diacetyl acyclovir by utilizing guanosine

A technology of diacetyl acyclovir and diacetyl guanine, which is applied in the field of synthesizing diacetyl acyclovir from guanosine, can solve problems such as overflow of reaction materials, improve safety, reduce processing costs, and reduce solubility Effect

Inactive Publication Date: 2020-07-03
通辽德胜生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method is relatively low, only 78.8%, and in the actual preparation of diacetylguanine, when guanosine and acetic anhydride react, the guanosine chain scission needs to absorb heat, and the chain scission releases heat instantly, so that the reaction material will overflow

Method used

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  • Method for synthesizing diacetyl acyclovir by utilizing guanosine
  • Method for synthesizing diacetyl acyclovir by utilizing guanosine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] (1) uniformly mix a part of acetic anhydride and guanosine to obtain a mixed solution 1; uniformly mix another part of acetic anhydride (equal to the acetic anhydride in the mixed solution 1) and boric acid, and heat up to 120° C. to obtain a mixed solution 2; Slowly add the mixed solution 1 to the mixed solution 2 at a rate of 5 cubic meters per hour, and keep it warm at 120°C for 6 hours after the addition, wherein the total amount of acetic anhydride in the guanosine, mixed solution 1 and mixed solution 2 The mass ratio of boric acid to boric acid is 1:6.6:0.008; then distill part of the acetic acid under the condition of slight negative pressure below 0.04MPA, the amount of distilled acetic acid is 25% of the total amount of acetic acid produced in theory, after the distillation is completed, keep warm at 120°C to continue React for 6.5 hours; after the reaction is completed, cool down to 4°C and filter or suction filter to collect the filter cake and filtrate; the f...

Embodiment 2

[0047] (1) uniformly mix a part of acetic anhydride and guanosine to obtain a mixed solution 1; uniformly mix another part of acetic anhydride (equal to the acetic anhydride in the mixed solution 1) and boric acid, and heat up to 125° C. to obtain a mixed solution 2; Slowly add the mixed solution 1 to the mixed solution 2 at a rate of 4 cubic meters per hour, and keep it warm at 125°C for 6 hours after the addition, wherein the total amount of acetic anhydride in the guanosine, mixed solution 1 and mixed solution 2 The mass ratio to boric acid is 1:6.6:0.008; then distill part of the acetic acid under the condition of a slight negative pressure below 0.04MPA, and the amount of distilled acetic acid is 20% of the total amount of acetic acid produced in theory. React for 6 hours; after the reaction is completed, cool down to 0°C and filter or suction filter to collect the filter cake and filtrate; the filter cake is further washed twice with acetic anhydride and dried in vacuum t...

Embodiment 3

[0053] (1) uniformly mix a part of acetic anhydride and guanosine to obtain a mixed solution 1; uniformly mix another part of acetic anhydride (equal to the acetic anhydride in the mixed solution 1) and boric acid, and heat up to 120° C. to obtain a mixed solution 2; Slowly add the mixed solution 1 to the mixed solution 2 at a rate of 6 cubic meters per hour. After the addition, keep the temperature at 120°C for 6.5 hours, wherein the total amount of guanosine, mixed solution 1 and mixed solution 2 is acetic anhydride. The mass ratio of boric acid to boric acid is 1:6.6:0.008; then part of the acetic acid is distilled under the condition of a slight negative pressure below 0.04MPA, and the amount of distilled acetic acid is 30% of the total amount of acetic acid produced in theory. After the distillation is completed, it is kept at 120°C Continue the reaction for 7 hours; after the reaction is completed, cool down to 5°C and filter or suction filter to collect the filter cake a...

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Abstract

The invention belongs to the field of organic synthesis, and particularly relates to a method for synthesizing diacetyl acyclovir by utilizing guanosine. The preparation method comprises the followingsteps: reacting acetic anhydride, guanosine and boric acid to obtain diacetyl guanine and tetra-acetyl ribose; carrying out reactions among diacetyl guanine, 2-oxa-1,4-butanediol diacetate and p-toluene sulfonic acid at 110-115 DEG C, and then purifying the reaction product to obtain a diacetyl acyclovir pure product. The method is simple in process and very beneficial to large-scale production of diacetyl acyclovir, the processing cost of diacetyl acyclovir can be greatly reduced, and the production efficiency of diacetyl acyclovir is improved.

Description

technical field [0001] The invention belongs to the field of organic synthesis, and in particular relates to a method for synthesizing diacetyl acyclovir from guanosine. Background technique [0002] Diacetyl-Aciclovir (Dicacetyl-Aciclovir), the molecular formula is C 12 h 15 N 5 o 5 , the molecular weight is 309.28, and the structural formula is as follows. Diacetyl acyclovir is an important intermediate for the synthesis of high-efficiency broad-spectrum antiviral drug acyclovir, wherein the latter is highly effective against type I and type II herpes simplex and varicella zoster virus. With the deepening of people's research, Acyclovir can also be used for anti-HIV virus. [0003] [0004] Currently, there are multiple methods for the synthesis of diacetyl acyclovir to be disclosed. in: [0005] CN110818715A specifically discloses: (1) add anhydrous toluene, diacetylguanine, p-toluenesulfonic acid to the reaction kettle, and heat up to reflux; (2) keep the tempe...

Claims

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Application Information

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IPC IPC(8): C07D473/18
CPCC07D473/18
Inventor 岳广宇王颖苏华强郝新红
Owner 通辽德胜生物科技有限公司
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