Method for preparing raw medicament of stable fenpyroximate

A technology of pyraclofen and tert-butyl, which is applied in the field of special-effect products for mites, and can solve problems such as the sales of pyraclofen active drug by Japan Agricultural Chemicals Co., Ltd.

Inactive Publication Date: 2008-10-01
北京绿色农华作物科技有限公司
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  • Abstract
  • Description
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  • Application Information

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Problems solved by technology

[0004] At present, only our company and Nippon Pesticide Co., Ltd. have obtained pesticide registration in my countr...

Method used

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  • Method for preparing raw medicament of stable fenpyroximate
  • Method for preparing raw medicament of stable fenpyroximate
  • Method for preparing raw medicament of stable fenpyroximate

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Embodiment Construction

[0014] The synthesis of pyraclofen is mainly: the synthesis of two intermediates of tert-butyl p-chloromethylbenzoate and 1,3-dimethyl-5-phenoxypyrazole-4-carboxylic acid aldoxime, and then the two The intermediate synthesis is a finished product of pyraclofen with a purity of ≥96%.

[0015] (1) Synthesis of tert-butyl p-chloromethylbenzoate

[0016] The synthesis of tert-butyl p-chloromethylbenzoate is mainly divided into three stages, which are respectively the synthesis of p-chloromethylbenzoic acid, p-chloromethylbenzoyl chloride, and tert-butyl p-chloromethylbenzoate.

[0017] 1) Synthesis of p-chloromethylbenzoic acid

[0018] Add chlorobenzene, catalyst A, and p-toluic acid into the reaction kettle, add sulfuryl chloride dropwise under reflux, drop the temperature after the dropwise addition, keep warm, filter, and recrystallize methanol to obtain p-chloromethylbenzoic acid.

[0019] ① Reactive formula

[0020]

[0021] 2) Synthesis of p-chloromethylbenzoyl chlori...

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Abstract

At present, most of the acaricides produced domestically or abroad are old varieties which mainly comprises propargite of sulfurous ester, kelthane of diphenyl carbinol, azocyclotin and fenbutatin xoide of organotin, pyridaben of heterocyclic compound and isocarbophos of organophosphorus, etc. Due to being used for a long time, the old varieties generate serious drug fastness in most regions and can be effective when being used in high dose. Therefore, the old varieties cannot satisfy the demands of market, and a new acaricide is needed to solve the problem. By aiming at the action of acaricides and combining the characteristics thereof, a novel acaricide of phenoxy pyrazoline esters is developed by the researchers of our company, that is fenpyroximate, which has the action of contact poisoning, and special effects on the egg, young acarids, nymph, adult acarids of acarids in every development phase, and can simultaneously and effectively treat plant diseases and insect pests such as diamondback moth, prodenia litura, Chilo suppressalis, rice fulgorid, barley powdery mildew, oat crown rust, and downy mildew of cucurbits, etc.

Description

technical field [0001] The invention relates to a method for preparing a stable fenpyroxate raw drug, in particular to a special-effect product for preventing and controlling mites on fruit trees such as citrus and apples and various crops. Background technique [0002] At present, most of the acaricides produced at home and abroad are sulfite-based clofenac (propargite), benzhydryl alcohol-based dicofol, organotin-based triazotin and fenbutyltin, and heterocyclic compounds. Pyridaben and organic phosphorus isocarbophos are mainly old varieties. Because these old varieties have been used for a long time, many varieties have developed high resistance, and they are only effective when used in large doses. Due to the long residual time of dicofol (the residue remains in the crops after one year of application), isocarbophos is a highly toxic pesticide, and it is a pesticide that is prohibited in green food production. It has been used for many years, and serious drug resistanc...

Claims

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Application Information

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IPC IPC(8): A01N43/56A01P7/02
Inventor 朱信阳徐宗跃陈垦
Owner 北京绿色农华作物科技有限公司
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