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Cyclic compound, preparation method and application thereof

A compound and solvate technology, applied in the field of cyclic compounds and their preparation, can solve the problems of reduced control effect of wheat powdery mildew, no wheat powdery mildew found, no compound found yet, etc.

Active Publication Date: 2022-01-18
SHANGHAI VIWIT PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as the use time goes on, due to the resistance to the agent, even if the amount of the agent is gradually increased, the control effect on wheat powdery mildew is gradually reduced (see: field efficacy test of different agents on the control of wheat powdery mildew .Yang Benxiang, Qin Jianhua, etc. Barley and Cereal Science.No.2.2014.); Therefore, it is necessary to continuously develop new compounds suitable as fungicides for the control of wheat powdery mildew, so as to better ensure the safety of food production
[0005] Up to now, no relevant reports on the compounds represented by the formula I of the present invention have been retrieved, and no relevant reports have been found on the use of the compounds represented by the formula I of the present invention as fungicides for the prevention and treatment of wheat powdery mildew

Method used

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  • Cyclic compound, preparation method and application thereof
  • Cyclic compound, preparation method and application thereof
  • Cyclic compound, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] Preparation Example 1, intermediate derivatives embodiment varenicline

[0108] Intermediate varenicline derivatives, production method comprising the steps of:

[0109]

[0110] Wherein, derivatives of A, B each other isomer;

[0111] (1) In the reaction flask, the 7,8-dinitro-2,3,4,5-tetrahydro-3- (trifluoroacetyl) -1,5-benzo-bridged -1H-3- azepine (intermediate varenicline, CAS number: 230615-59-5) 5g of isopropyl alcohol was added to (75 mL) and water (25mL) mixed solution was added palladium on carbon (Pd / C, Pd 5wt %, a water content 46.5wt%,) 0.5g, later replaced by hydrogen, hydrogen gas is continued, the reaction was stirred for 7 days at room temperature (reaction temperature may be 10 ℃ ~ 40 ℃, preferably 15 ℃ ~ 30 ℃), to obtain a reaction solution;

[0112] (2) The reaction solution was filtered through celite pad, and the filtrate rotary evaporated, the remainder was concentrated to approximately 30mL, was added and extracted with dichloromethane, the organi...

Embodiment 2

[0123] 2, the wheat powdery mildew Test Example

[0124] Test guidelines to China Agricultural industry standard NY / T 1156.4-2006 Pesticide indoor biocides Part 4: Wheat Powdery Mildew Control Test method potted wheat varieties: Luyuandan 502 were measured A derivative of the present invention, derivative B activity and powdery mildew control effect to 97% of prothioconazole, 42% metrafenone, water as a control.

[0125] The test results, shown in Table 2.

[0126] Wheat Powdery Mildew Control Test results Table 2

[0127]

[0128]

[0129] The above results show that the derivatives of the present invention A, B derivatives, the drug concentration at 400mg / L, and show some powdery mildew control effect, particularly in the reagent concentration 1000mg / L, and wheat powdery mildew control effect can reach 100%.

Embodiment 3

[0130] 3, rice sheath blight control test Example

[0131] Test guidelines to China Agricultural industry standard NY / T 1156.5-2006 Pesticide indoor biocides Part 5: inhibition of Rhizoctonia Vicia test method A derivatives of the present invention were measured, derivative B Rhizoctonia activity and control effect to 97% prothioconazole, penflufen, water as a control.

[0132] The test results, shown in Table 3.

[0133] Table 3 rice sheath blight control test results

[0134]

[0135] The above results show that the derivatives of the present invention A, B derivatives, the drug concentration at 1000mg / L, and Rhizoctonia exhibited a preventive effect.

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Abstract

The invention belongs to the field of compounds, and particularly discloses a cyclic compound as shown in a formula I or a pharmaceutically acceptable salt, a crystal form and a solvate thereof, wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, deuterium, tritium, hydroxyl, sulfydryl, amino and the like, and R11, R12, R13, R14, R15 and R16 are independently selected from hydrogen, deuterium, tritium, hydroxyl, sulfydryl, amino and the like. The invention also discloses a preparation method of the compound as shown in the formula I, application of the compound as a bactericide and / or an insecticide, a pesticide composition and an intermediate compound of the compound. The compound disclosed by the invention is novel and unique in structure, shows different degrees of prevention and control effects on wheat powdery mildew, rice sheath blight disease, aphid, plutella xylostella and other pathogenic bacteria or insect pests, is expected to be popularized and applied as a bactericide and / or an insecticide, and provides a new potential choice for agricultural pesticide application.

Description

Technical field [0001] The invention belongs to the field of compounds, and involves cyclic compounds and preparation methods and applications thereof. Background technique [0002] Wheat white powder is a worldwide disease, which is distributed in major production. my country's Shandong, Sichuan, Guizhou, and Yunnan have generally harmful harm. In recent years, the disease has been in the northeast, North China and northwest tomorrow, and has become increasingly serious. The disease can infringe on the upper organs of wheat plants, with blade and leaf sheath as the master, and the incidence of morphine and housing can also be injured. The general year of the disease can reduce production by 5% to 10%, and when severely reduced production, it is more than 30%, and the safety of food production is harmful. [0003] At this stage, the main prevention and treatment methods for wheat powder disease are: Breeding disease-resistant varieties, using chemicals such as triazole fungicides...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D257/10A01N43/713A01P3/00A01P7/04C07D221/22
CPCC07D257/10A01N43/713C07D221/22
Inventor 魏彦君王建杨猛拉杰斯·萨胡邢艳平刘希望徐青景
Owner SHANGHAI VIWIT PHARMA CO LTD