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METHOD FOR ASYMMETRICALLY CATALYZED SYNTHESIS OF NITROPYRAZOLE AMIDE COMPOUND 发明申请

2023-10-20 3670 755K 0

专利信息

申请日期 2025-07-09 申请号 WOCN15081341
公开(公告)号 WO2016045415A1 公开(公告)日 2016-03-31
公开国别 WO 申请人省市代码 全国
申请人 ZHEJIANG JIUZHOU PHARMACEUTICAL CO LTD
简介 A method for asymmetrically catalyzed synthesis of a γ-nitropyrazole amide compound, where a nitroalkene and an α, β-unsaturated pyrazole amide are employed as raw materials, a complex formed by a chiral amine oxide and a rare earth metal compound serves as a catalyst, a 4 Å molecular sieve serves as an additive, and the γ-nitropyrazole amide compound is produced after a reaction, which has a yield as high as 99% and an enantiomeric excess as high as 99% ee. The catalytic system not only has the advantages of a simple operation, mild reaction conditions, not requiring any acidic/basic additive, convenient product purification, high yield and enatioselectivity, compliance with green atomic economy, and great prospects for industrial application, but also allows the γ-nitropyrazole amide compound produced via the reaction to undergo some simple chemical conversions to produce some molecules having physiological activities.


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