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

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

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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Veröffentlicht in:Synthetic communications 1998-12, Vol.28 (23), p.4419-4429
Hauptverfasser: Lila, Christine, Gloanec, Philippe, Cadet, Laurence, Hervé, Yolande, Fournier, Jean, Leborgne, Fabrice, Verbeuren, Tony J., DeNanteuil, Guillaume
Format: Artikel
Sprache:eng
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Zusammenfassung: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.
ISSN:0039-7911
1532-2432
DOI:10.1080/00397919808004477