2015Unpublished venueRequires access

Synthetic Process of Novel Pesticides Cyclaniliprole

Liu An-chan

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Abstract

[Aims]This paper aims to improve synthetic process and to raise yield of cyclaniliprole.[Methods]1-Cyclopropyl methyl keton was reacted with formamide in the present of formic acid,followed by hydrochloric acid hydrolysis to give 1-cyclopropylethylamine.Then 2-amino-3-bromo-chloro-N-(1-cyclopropyl-ethyl)benzamide was prepared by the reaction of 5-chloro-2-nitrobenzic acid with 1-cyclopropylethyl amine,followed by nitro reduction with iron powder,brominated with bromine;cyclaniliprole was achieved from 3-bromo-1-(3-chloro-2-pyridinyl)-~1H-pyrazole-5-carboxylic acid and 2-amino-3-bromo-chloro-N-(1-cyclopropylethyl)benzamide by dropping methanesulfonyl chloride at 0-5 ℃The total yield was 27%and the purity of the production was 96.1%.[Results]The product thus obtained was identified with ~1H-NMR.[Conclusions]This process is simple,warm and economical,which is suitable for industrial scale manufacture.

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[Aims]This paper aims to improve synthetic process and to raise yield of cyclaniliprole.[Methods]1-Cyclopropyl methyl keton was reacted with formamide in the present of formic acid,followed by hydrochloric acid hydrolysis to give 1-cyclopropylethylamine.Then 2-amino-3-bromo-chloro-N-(1-cyclopropyl-ethyl)benzamide was prepared by the reaction of 5-chloro-2-nitrobenzic acid with 1-cyclopropylethyl amine,followed by nitro reduction with iron powder,brominated with bromine;cyclaniliprole was achieved from 3-bromo-1-(3-chloro-2-pyridinyl)-~1H-pyrazole-5-carboxylic acid and 2-amino-3-bromo-chloro-N-(1-cyclopropylethyl)benzamide by dropping methanesulfonyl chloride at 0-5 ℃The total yield was 27%and the purity of the production was 96.1%.[Results]The product thus obtained was identified with ~1H-NMR.[Conclusions]This process is simple,warm and economical,which is suitable for industrial scale manufacture.

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Available abstract

[Aims]This paper aims to improve synthetic process and to raise yield of cyclaniliprole.[Methods]1-Cyclopropyl methyl keton was reacted with formamide in the present of formic acid,followed by hydrochloric acid hydrolysis to give 1-cyclopropylethylamine.Then 2-amino-3-bromo-chloro-N-(1-cyclopropyl-ethyl)benzamide was prepared by the reaction of 5-chloro-2-nitrobenzic acid with 1-cyclopropylethyl amine,followed by nitro reduction with iron powder,brominated with bromine;cyclaniliprole was achieved from 3-bromo-1-(3-chloro-2-pyridinyl)-~1H-pyrazole-5-carboxylic acid and 2-amino-3-bromo-chloro-N-(1-cyclopropylethyl)benzamide by dropping methanesulfonyl chloride at 0-5 ℃The total yield was 27%and the purity of the production was 96.1%.[Results]The product thus obtained was identified with ~1H-NMR.[Conclusions]This process is simple,warm and economical,which is suitable for industrial scale manufacture.

Key concepts: Benzamide, Chemistry, Yield (engineering), Hydrolysis, Hydrochloric acid, Formic acid, Bromine, Formamide

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