Preparation of amides from an acid and amine for intermediates in the synthesis of morphinans
US8461384B2 · kind B2 · utility
0Cited by
3References
14Claims
0Family size
Assignee
Inventors
Key dates
| Filing date | Jun 10, 2009 |
| Grant date | Jun 11, 2013 |
| Priority date | — |
| Expiry date | Nov 13, 2030 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.