Invention Grant
- Patent Title: Method for synthesizing 3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxylic acid and intermediates thereof
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Application No.: US16325717Application Date: 2016-09-29
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Publication No.: US10556868B2Publication Date: 2020-02-11
- Inventor: Renbao He , Yingmei Wang , Hongming Shao , Yizhong Jin
- Applicant: ZHEJIANG YONGTAI TECHNOLOGY CO., LTD.
- Applicant Address: CN Zhejiang
- Assignee: ZHEJIANG YONGTAI TECHNOLOGY CO., LTD.
- Current Assignee: ZHEJIANG YONGTAI TECHNOLOGY CO., LTD.
- Current Assignee Address: CN Zhejiang
- Agency: JCIP Global Inc.
- Priority: CN201610668266 20160815
- International Application: PCT/CN2016/100717 WO 20160929
- International Announcement: WO2018/032586 WO 20180222
- Main IPC: C07D231/28
- IPC: C07D231/28 ; C07D231/14

Abstract:
The present invention relates to a method for synthesizing a compound of 3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxylic acid, wherein including the steps of: (A) the diethyl ester compounds represented by the following Formula IV are reacted under the action of amine, alkali and carbonyl reagents to produce the acrylic diester compound represented by the following Formula I, wherein: (B) the above compound represented by the Formula I is reacted with a fluoride reagent, a Lewis acid and a methyl hydrazine to form a pyrazole ring-containing diester compound represented by the Formula II, (C) the heterocyclic-containing diester compound represented by the Formula II is reacted with a base to give 3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxylic acid represented by the Formula III.
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