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US08445682B2 Preparation of 3,4-dihydroisoquinolines from an acid and an amine 有权
由酸和胺制备3,4-二氢异喹啉

Preparation of 3,4-dihydroisoquinolines from an acid and an amine
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.
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