Invention Grant
- Patent Title: Preparation of 3,4-dihydroisoquinolines from an acid and an amine
- Patent Title (中): 由酸和胺制备3,4-二氢异喹啉
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Application No.: US12518434Application Date: 2007-12-10
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Publication No.: US08445682B2Publication Date: 2013-05-21
- Inventor: Christopher W. Grote , Peter X. Wang , Frank W. Moser , Gary L. Cantrell
- Applicant: Christopher W. Grote , Peter X. Wang , Frank W. Moser , Gary L. Cantrell
- Applicant Address: US MO Hazelwood
- Assignee: Mallinckrodt LLC
- Current Assignee: Mallinckrodt LLC
- Current Assignee Address: US MO Hazelwood
- International Application: PCT/US2007/025263 WO 20071210
- International Announcement: WO2008/073390 WO 20080619
- Main IPC: C07D217/00
- IPC: C07D217/00

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
- US20100063290A1 Preparation of 3,4-Dihydroisoquinolines from an Acid and an Amine Public/Granted day:2010-03-11
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