Invention Grant
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
- Patent Title: Preparation of 3,4-dihydroisoquinolines in the synthesis of morphinans
- Patent Title (中): 吗啡喃合成中3,4-二氢异喹啉的制备
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Application No.: US12482014Application Date: 2009-06-10
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Publication No.: US08232400B2Publication Date: 2012-07-31
- Inventor: Peter X. Wang , Frank W. Moser , Christopher W. Grote , Gary L. Cantrell
- Applicant: Peter X. Wang , Frank W. Moser , Christopher W. Grote , Gary L. Cantrell
- Applicant Address: US MO Hazelwood
- Assignee: Mallinckrodt LLC
- Current Assignee: Mallinckrodt LLC
- Current Assignee Address: US MO Hazelwood
- Main IPC: C07D217/02
- IPC: C07D217/02
Abstract:
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.
Public/Granted literature
- US20090247761A1 Preparation of 3,4-Dihydroisoquinolines in the Synthesis of Morphinans Public/Granted day:2009-10-01
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