Invention Grant
- Patent Title: Process for preparing pyridinamines and novel polymorphs thereof
- Patent Title (中): 制备吡啶胺及其新型多晶型物的方法
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Application No.: US13444833Application Date: 2012-04-11
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Publication No.: US08648203B2Publication Date: 2014-02-11
- Inventor: Shlomi Cohen , Sharona Zamir
- Applicant: Shlomi Cohen , Sharona Zamir
- Applicant Address: IL Beer Sheva
- Assignee: Makhteshim Chemical Works Ltd.
- Current Assignee: Makhteshim Chemical Works Ltd.
- Current Assignee Address: IL Beer Sheva
- Agency: Browdy and Neimark, PLLC
- Priority: IL172137 20051123; IL172685 20051219
- Main IPC: A61K31/44
- IPC: A61K31/44 ; C07D213/72

Abstract:
The present invention relates to an improved process for the synthesis and purification of 3-chloro-N-(3-chloro-5-tri-fluoromethyl-2-pyridyl)-α,α,α-trifluoro-2,6-di-nitro-p-toluidine (fluazinam) and other pyridinamines, which implements methyl isobutyl ketone (MIBK) as the reaction solvent. The process of the invention overcomes the drawbacks of prior art methods, by reducing the side reactions such as hydrolysis, eliminating the need for difficult and labor-intensive purification methods, and providing pure products in higher yields. The present invention relates to novel crystalline polymorphic forms fluazinam, and to mixtures of the polymorphs. The present invention also provides methods for preparing the novel polymorphs, as well as pharmaceutical compositions comprising same, and methods of using the polymorphs as pesticidal agents for combating noxious living organisms on agricultural and horticultural crops.
Public/Granted literature
- US20120197023A1 PROCESS FOR PREPARING PYRIDINAMINES AND NOVEL POLYMORPHS THEREOF Public/Granted day:2012-08-02
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