Large Scale Preparation of Protected 4-Aminomethylbenzamidine. Application to The Synthesis of the Thrombin Inhibitor,Melagatran |
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| Authors: | Christine Lila Philippe Gloanec Laurence Cadet Yolande Hervé Jean Fournier Fabrice Leborgne |
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| Institution: | 1. Institut de Recherche Servier , 11 rue des Moulineaux, Suresnes, 92150, France;2. ORIL Industrie , 13 rue Auguste Desgenetais, Bolbec, 76120, France |
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| Abstract: | To allow the preparation of melagatran on a multigram scale, we have investigated several approaches for the synthesis of the key intermediate 4-aminomethylbenzamidine. The only industrially suitable pathway relies on the preparation of an N-hydroxyimino intermediate. |
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