Process and intermediates for making substituted aspartic...

C - Chemistry – Metallurgy – 07 – D

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C07D 307/32 (2006.01) C07D 307/33 (2006.01) C07D 307/66 (2006.01) C07F 9/535 (2006.01) C07F 9/655 (2006.01)

Patent

CA 2402128

Disclosed herein is a method for making compounds that are useful as caspase inhibitor prodrugs of formula (I), wherein R1 is an optionally substituted group selected from an aliphatic group, aralkyl group, heterocyclylalkyl group or aryl group, and R2 is preferably a P2-P4 moiety of a caspase inhibitor. Key intermediates include the azidolactones (III) and (VIII).

L'invention concerne un procédé de préparation de composés, utiles en tant que promédicaments d'inhibition de la caspase, et correspondant à la formule (I) dans laquelle R?1¿ représente un groupe éventuellement substitué, choisi dans l'ensemble constitué par un groupe aliphatique, un groupe aralkyle, un groupe hétérocyclylalkyle ou un groupe aryle, R?2¿ représentant, de préférence, une fraction P¿2?-P¿4? d'un inhibiteur de caspase. L'invention concerne également des intermédiaires clés comprenant les azidolactones correspondant aux formules (III) et (VIII).

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