- 专利标题： METHOD FOR SYNTHESIZING 3-(DIFLUOROMETHYL)-1-METHYL-1H-PYRAZOLE-4-CARBOXYLIC ACID, AND INTERMEDIATES THEREOF
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申请号： EP16913341.0申请日： 2016-09-29
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公开(公告)号： EP3498695A1公开(公告)日： 2019-06-19
- 发明人: HE, Renbao , WANG, Yingshu , SHAO, Hongming , JIN, Yizhong
- 申请人： Zhejiang Yongtai Technology Co., Ltd.
- 申请人地址： No.1 5th Donghai Avenue Zhejiang Provincial Chemical and Medical Raw Materials Base Linhai Zone Zhejiang 317016 CN
- 专利权人： Zhejiang Yongtai Technology Co., Ltd.
- 当前专利权人： Zhejiang Yongtai Technology Co., Ltd.
- 当前专利权人地址： No.1 5th Donghai Avenue Zhejiang Provincial Chemical and Medical Raw Materials Base Linhai Zone Zhejiang 317016 CN
- 代理机构： Cabinet Chaillot
- 优先权： CN201610668266 20160815
- 国际公布： WO2018032586 20180222
- 主分类号： C07D231/14
- IPC分类号： C07D231/14
摘要：
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 :
R 1 =
R 2 =
(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.
(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 :
R 1 =
R 2 =
(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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