Synthesis of himbacine analogs

C - Chemistry – Metallurgy – 07 – D

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C07D 405/08 (2006.01) C07D 307/88 (2006.01) C07D 493/10 (2006.01)

Patent

CA 2594741

The present invention relates to an improved process for preparing imbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. An example of a step in the synthesis of such a himbacine analog is as follows: Formula (I)

La présente invention porte sur un procédé de préparation amélioré des analogues de l'himbacine. Les composés sont utiles comme antagonistes du récepteur de la thrombine. Ce procédé amélioré permet de réaliser plus facilement la purification par cristallisation, d'obtenir une meilleure scalabilité et un meilleur rendement de l'énantiomère désiré. L'invention porte également sur un exemple (I) d'une étape de synthèse de cet analogue de l'himbacine.

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