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US 2012/0238746 A1Published application
Processes and Intermediates for Preparing a Macrocyclic Protease Inhibitor of HCV
AssigneeJanssen R&D Ireland
InventorsAndras Horvath, Dominique Paul Michel Depré, Dominic John Ormerod
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Abstract
The present invention relates to synthesis procedures and intermediates of a compound of formula: and the salts thereof.
Claims26
1-32. (canceled)
A process for preparing a compound of formula (XVII) starting from an intermediate (XIV), followed by cyclization to obtain an intermediate (XV), followed by hydrolysis to the macrocyclic acid (XVI);
- followed by coupling with cyclopropylsulfonylamide in an amide forming reaction, thus obtaining the end product (XVII), as outlined in the following reaction scheme:
- and wherein the compound of formula (XIV) is prepared by a process starting from an intermediate (XI), which is hydrolysed to the acid (XII), which in turn is coupled with the cyclopropylamino acid ester (XIII) to obtain the desired end product (XIV), as outlined in the following reaction scheme:
- wherein R is C1-4alkyl, and R1, independently from R, is also C1-4alkyl.
Dependencies are inferred from the claim text.