Asymmetrically catalyzed synthesis method of nitropyrazole amide compound
AssigneeZhejiang Jiuzhou Pharmaceutical Co., Ltd.
InventorsXiaoming FENG, Qian YAO, Xiaohua LIU, Lili LIN, Yuheng ZHANG
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AssigneeZhejiang Jiuzhou Pharmaceutical Co., Ltd.
InventorsXiaoming FENG, Qian YAO, Xiaohua LIU, Lili LIN, Yuheng ZHANG
Estimating the term…
A synthesis method of γ-nitropyrazole amide compound through asymmetrical catalyzing technique is provided, a nitroalkane and an α,β-unsaturated pyrazole amide are applied as the raw material, a complex formed by a chiral amine oxide with a rare earth metal compound is served as the catalyst, a 4 Å molecular sieve is served as an additive, the γ-nitropyrazole amide compound can be obtained with a yield more than 99% and enantiomeric excess more than 99% ee. The catalytic system not only has the advantages of simple operation, mild reaction conditions, requiring no acid/base additives, convenient product purification, high yield and enatioselectivity, compliance with green atomic economy, and promising prospects for industrial application, but also allows the obtained γ-nitropyrazole amide compound to undergo some simple chemical conversions to produce some molecules having physiological activities.
An asymmetrically catalyzed synthesis method of a γ-nitropyrazole amide compound, wherein, in the reaction that a nitroalkane and an α,β-unsaturated pyrazole amide are employed as raw materials, a complex formed by a chiral amine oxide with a rare earth metal compound is served as a catalyst, a 4 Å molecular sieve is served as an additive, after the reaction finished, to obtain a γ-nitropyrazole amide compound, wherein,
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