Large Scale Preparation of Protected 4-Aminomethylbenzamidine. Application to The Synthesis of the Thrombin Inhibitor, Melagatran

Christine Lila Institut de Recherche Servier, 11 rue des Moulineaux, Suresnes, 92150, France

Philippe Gloanec Institut de Recherche Servier, 11 rue des Moulineaux, Suresnes, 92150, France

Laurence Cadet Institut de Recherche Servier, 11 rue des Moulineaux, Suresnes, 92150, France

Yolande Hervé ORIL Industrie, 13 rue Auguste Desgenetais, Bolbec, 76120, France

Jean Fournier ORIL Industrie, 13 rue Auguste Desgenetais, Bolbec, 76120, France

Fabrice Leborgne ORIL Industrie, 13 rue Auguste Desgenetais, Bolbec, 76120, France

Tony J. Verbeuren Institut de Recherche Servier, 11 rue des Moulineaux, Suresnes, 92150, France

Guillaume DeNanteuil Institut de Recherche Servier, 11 rue des Moulineaux, Suresnes, 92150, 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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Large Scale Preparation of Protected 4-Aminomethylbenzamidine. Application to The Synthesis of the Thrombin Inhibitor, Melagatran

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Large Scale Preparation of Protected 4-Aminomethylbenzamidine. Application to The Synthesis of the Thrombin Inhibitor, Melagatran

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