Preparation of 3,4-dihydroisoquinolines from an acid and an amine
US8445682B2 · kind B2 · utility
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20Claims
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Key dates
| Filing date | Dec 10, 2007 |
| Grant date | May 21, 2013 |
| Priority date | — |
| Expiry date | Sep 10, 2029 |
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.