基本信息:
- 专利标题： PROCESS FOR MAKING CGRP RECEPTOR ANTAGONISTS
- 专利标题（中）：制备CGRP受体拮抗剂的方法
- 申请号：PCT/US2013/030692 申请日：2013-03-13
- 公开(公告)号：WO2013169348A1 公开(公告)日：2013-11-14
- 发明人： CHEN, Frank , MOLINARO, Carmela , WUELFING, W. Peter , YASUDA, Nobuyoshi , YIN, Jianguo , ZHONG, Yong-Li , LYNCH, Joseph , ANDREANI, Teresa
- 申请人： MERCK SHARP & DOHME CORP. , CHEN, Frank , MOLINARO, Carmela , WUELFING, W. Peter , YASUDA, Nobuyoshi , YIN, Jianguo , ZHONG, Yong-Li , LYNCH, Joseph , ANDREANI, Teresa
- 申请人地址： 126 East Lincoln Avenue Rahway, New Jersey 07065-0907 US
- 专利权人： MERCK SHARP & DOHME CORP.,CHEN, Frank,MOLINARO, Carmela,WUELFING, W. Peter,YASUDA, Nobuyoshi,YIN, Jianguo,ZHONG, Yong-Li,LYNCH, Joseph,ANDREANI, Teresa
- 当前专利权人： MERCK SHARP & DOHME CORP.,CHEN, Frank,MOLINARO, Carmela,WUELFING, W. Peter,YASUDA, Nobuyoshi,YIN, Jianguo,ZHONG, Yong-Li,LYNCH, Joseph,ANDREANI, Teresa
- 当前专利权人地址： 126 East Lincoln Avenue Rahway, New Jersey 07065-0907 US
- 代理机构： MERCK SHARP & DOHME CORP.
- 优先权： US61/644,631 20120509
- 主分类号： A01N43/90
- IPC分类号： A01N43/90 ; A61K31/519
摘要：
The disclosure encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, having less steps and improved yields as compared to previous synthetic methods for making these compounds, which are CGRP receptor antagonists, useful for the treatment of migrane. Conditions for an amide bond formation between an acid and amine include for example reacting the compounds of Formulae B (after salt break) and C with an amide coupling reagent and optionally an additive and an acid and/or a base in a non-reactive solvent.
摘要（中）：
本发明涉及制备哌啶酮羧酰胺二氢化茚和吖烷烷衍生物的新方法，与用于制备这些化合物的合成方法相比，其具有较少的步骤和提高的产率，这些化合物是可用于治疗迁移物的CGRP受体拮抗剂。 在酸和胺之间形成酰胺键的条件包括例如使式B化合物（盐分后）和C与酰胺偶联剂和任选的添加剂和酸和/或碱在非反应性溶剂中反应 。