C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 235/34 (2006.01) C07C 231/02 (2006.01) C07C 303/30 (2006.01) C07C 309/66 (2006.01)
Patent
CA 2674099
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, POCI3 that is necessary to form the 3,4-dihydroisoquinoline.
Cantrell Gary L.
Grote Christopher W.
Moser Frank W.
Wang Peter X.
Mallinckrodt Inc.
Mallinckrodt Llc
Osler Hoskin & Harcourt Llp
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