- 专利标题: Method for producing fluorine-containing cyclopropane carboxylic acid compound
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申请号: US15741020申请日: 2016-06-24
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公开(公告)号: US10450291B2公开(公告)日: 2019-10-22
- 发明人: Takashi Kashiwaba , Takako Yamazaki , Shoko Ishii , Shunsuke Mimura , Masanori Fushimi , Ryuichi Okamoto , Haruki Kobayashi , Manabu Yasumoto
- 申请人: Central Glass Company, Limited
- 申请人地址: JP Ube-shi
- 专利权人: Central Glass Company, Limited
- 当前专利权人: Central Glass Company, Limited
- 当前专利权人地址: JP Ube-shi
- 代理机构: Crowell & Moring LLP
- 优先权: JP2015-129628 20150629
- 国际申请: PCT/JP2016/068748 WO 20160624
- 国际公布: WO2017/002712 WO 20170105
- 主分类号: C07D327/10
- IPC分类号: C07D327/10 ; C07C67/313 ; C07C67/343 ; C07C67/52 ; C07C69/74 ; C07C67/08 ; C07C211/27 ; C07B57/00
摘要:
The present invention provides an industrially applicable method for production of a fluorine-containing cyclopropane carboxylic acid compound useful as an intermediate for pharmaceutical and agrichemical products. A fluorine-containing cyclopropane monoester is obtained by: forming a fluorine-containing cyclic sulfate with the use of a fluorine-containing dial compound and sulfuryl fluoride (as a cyclic sulfuric esterification step); reacting the fluorine-containing cyclic sulfate with a malonic diester, thereby forming a fluorine-containing cyclopropane diester (as a cyclopropanation step); and hydrolyzing the fluorine-containing cyclopropane diester (as a hydrolysis step). The fluorine-containing cyclopropane carboxylic acid compound, such as fluorine-containing cyclopropane monoester or its salt, can be obtained with high chemical and optical purity by mixing the fluorine-containing cyclopropane monoester with an amine and subjecting the resulting salt of the fluorine-containing cyclopropane monoester and amine to recrystallization purification.
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