发明申请
- 专利标题: Preparation of 3,4-Dihydroisoquinolines from an Acid and an Amine
- 专利标题(中): 从酸和胺制备3,4-二氢异喹啉
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申请号: US12518434申请日: 2007-12-10
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公开(公告)号: US20100063290A1公开(公告)日: 2010-03-11
- 发明人: Christopher W. Grote , Peter X. Wang , Frank W. Moser , Gary L. Cantrell
- 申请人: Christopher W. Grote , Peter X. Wang , Frank W. Moser , Gary L. Cantrell
- 国际申请: PCT/US07/25263 WO 20071210
- 主分类号: C07D217/00
- IPC分类号: C07D217/00
摘要:
The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl3 that is necessary to form the 3,4-dihydroisoquinoline.
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