Preparation of (s)-decahydroisoquinoline-3-carboxylic acid...

C - Chemistry – Metallurgy – 07 – D

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C07D 217/26 (2006.01)

Patent

CA 2238478

Methods for preparing (S)-N-tert-butyl-1,2,3,4-tetrahydro-3-isoquinoline- carboxamide ("tic-c"), and converting tic-c to (S)-decahydroisoquinoline-3- carboxylic acid t-butylamide ("tic-d") are disclosed. The initial step in the formation of tic-c involves the phosgenation of a substituted tetrahydroisoquinoline to form an N-carboxy anhydride. Tic-d is used as an intermediate in the synthesis of known compounds having pharmaceutical activity.

Cette invention concerne des procédés de préparation de (S)-N-tert-butyl-1,2,3,4-tétrahydro-3-isoquinoline-carboxamide ("tic-c") et de conversion de tic-c en (S)-décahydro-isoquinoline-3-acide carboxylique T-butylamide ("tic-d"). L'étape initiale de la préparation de tic-c consiste en une phosgénation d'une tétrahydro-isoquinoline substituée en vue de l'obtention d'un N-carboxy anhydride. Le tic-d est utilisé en tant qu'intermédiaire dans la synthèse de composés connus dotés d'une activité pharmaceutique.

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