发明授权
US08232400B2 Preparation of 3,4-dihydroisoquinolines in the synthesis of morphinans
有权
吗啡喃合成中3,4-二氢异喹啉的制备
- 专利标题： Preparation of 3,4-dihydroisoquinolines in the synthesis of morphinans
- 专利标题（中）： 吗啡喃合成中3,4-二氢异喹啉的制备
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申请号： US12482014申请日： 2009-06-10
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公开(公告)号： US08232400B2公开(公告)日： 2012-07-31
- 发明人: Peter X. Wang , Frank W. Moser , Christopher W. Grote , Gary L. Cantrell
- 申请人： Peter X. Wang , Frank W. Moser , Christopher W. Grote , Gary L. Cantrell
- 申请人地址： US MO Hazelwood
- 专利权人： Mallinckrodt LLC
- 当前专利权人： Mallinckrodt LLC
- 当前专利权人地址： US MO Hazelwood
- 主分类号： C07D217/02
- IPC分类号： C07D217/02
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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