Methods and intermediates for synthesis of selective dpp-iv...

Details Methods and intermediates for synthesis of selective dpp-iv... Methods and intermediates for synthesis of selective dpp-iv...

C - Chemistry, Metallurgy

07

D

C07D 207/14 (2006.01) C07F 5/02 (2006.01)

Patent

CA 2680133

Methods and intermediates for the synthesis of selective inhibitors of dipeptidyl peptidase IV (DPP-IV) are provided. Coupling of a carboxylate salt with a boro-proline derivative provides a protected form of a DPP-IV inhibitor, which may be deblocked to yield the medicinal compound. The carboxylate salt can be a crystalline form of a sodium salt or a dicyclohexylammonium salt. The inhibitor can be used in the treatment of diabetes.

L'invention concerne des procédés et des intermédiaires pour la synthèse d'inhibiteurs sélectifs de la dipeptidyle peptidase IV (DPP-IV). Le couplage d'un sel de carboxylate avec un dérivé de boro-proline fournit une forme protégée d'un inhibiteur de DPP-IV, qui peut être débloquée pour obtenir le composé médicinal. Le sel de carboxylate peut être une forme cristalline d'un sel de sodium ou d'un sel de dicyclohexylammonium. L'inhibiteur peut être utilisé pour le traitement du diabète.

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