发明授权
US08633321B2 Synthesis of (4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester and intermediates thereof
有权
（4-氟-3-哌啶-4-基 - 苄基） - 氨基甲酸叔丁酯的合成及其中间体
- 专利标题： Synthesis of (4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester and intermediates thereof
- 专利标题（中）： （4-氟-3-哌啶-4-基 - 苄基） - 氨基甲酸叔丁酯的合成及其中间体
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申请号： US13426721申请日： 2012-03-22
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公开(公告)号： US08633321B2公开(公告)日： 2014-01-21
- 发明人: Nakyen Choy , John J. Shay, Jr. , Adam W. Sledeski
- 申请人： Nakyen Choy , John J. Shay, Jr. , Adam W. Sledeski
- 申请人地址： US NJ Bridgewater
- 专利权人： Sanofi-Aventis U.S. LLC
- 当前专利权人： Sanofi-Aventis U.S. LLC
- 当前专利权人地址： US NJ Bridgewater
- 代理商 Ronald G. Ort
- 主分类号： C07D211/02
- IPC分类号： C07D211/02
摘要：
The present invention is an improved method for the preparation of (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester, compound of formula I. The invention is directed to a method of synthesis for the compound of formula I in three steps, comprising formation of 5-((tert-butoxycarbonyl)aminomethyl)-2-fluorobenzeneboronic acid (compound 11), reaction of compound 11 under Suzuki coupling conditions to yield (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester and selective hydrogenation of the aforementioned product under hydrogenation conditions yields compound I. The invention is also directed to the intermediates 5-((tert-butoxycarbonyl)amino-methyl)-2-fluorobenzeneboronic acid (compound 11), and (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester (compound 13).
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