Processes and Intermediates for Preparing a Macrocyclic Protease Inhibitor of HCV
AssigneeJanssen Pharmaceutica NV
InventorsAndras Horvath, Dominic John Ormerod, Dominique Paul Michel Depre, Veronique Cerpentier
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Abstract
The present invention relates to the cinchonidine salt useful in the preparation of intermediates for preparing a macrocyclic HCV inhibitor, as well as processes involving this salt.
Claims15
A process for preparing a compound of formula (VIII), starting from an cinchonidine salt (XXa), which is reacted with N-methyl-hexenamine (NMHA) (XIX) in an amide-forming reaction to yield the bicyclic lactone amide (XVIII), in which the lactone group is opened to yield the desired product (VIII), as illustrated in the scheme below, wherein R1 is C1-4alkyl:
A process for preparing the cinchonidine salt (XXa), which is obtained from the racemic salt (XX) by crystallization:
The cinchonidine salt of formula
Dependencies are inferred from the claim text.