Large scale preparation of protected 4-aminomethylbenzamidine. Application to the synthesis of the thrombin inhibitor, melagatran

Article abstract of DOI:10.1080/00397919808004477

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

Full text of DOI:10.1080/00397919808004477

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Large Scale Preparation
of Protected 4-
Aminomethylbenzamidine.
Application to The Synthesis
of the Thrombin Inhibitor,
Melagatran
Christine Lila a , Philippe Gloanec a , Laurence
Cadet a , Yolande Hervé b , Jean Fournier b
, Fabrice Leborgne b , Tony J. Verbeuren a
Guillaume DeNanteuil a
&
a Institut de Recherche Servier , 11 rue des
Moulineaux, Suresnes, 92150, France
b ORIL Industrie , 13 rue Auguste Desgenetais,
Bolbec, 76120, France
Published online: 23 Aug 2006.
To cite this article: Christine Lila , Philippe Gloanec , Laurence Cadet ,
Yolande Hervé , Jean Fournier , Fabrice Leborgne , Tony J. Verbeuren
& Guillaume DeNanteuil (1998) Large Scale Preparation of Protected 4-
Aminomethylbenzamidine. Application to The Synthesis of the Thrombin
Inhibitor, Melagatran, Synthetic Communications: An International Journal for
Rapid Communication of Synthetic Organic Chemistry, 28:23, 4419-4429, DOI:
10.1080/00397919808004477
To link to this article: http://dx.doi.org/10.1080/00397919808004477

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