Process for the preparation of heterocyclic ester derivatives

摘要

The present invention is directed to a process for the preparation of heterocyclic ester derivatives of formula I;
wherein A1, SEM, and W1 are as defined herein. Such compounds are useful as intermediates in the synthesis of derivatives useful as protein tyrosine kinase inhibitors, more particularly inhibitors of c-fms kinase.

主权项

1. A process for the preparation of a compound of formula A1 is selected from the group consisting of C1-2 alkyl; or a pharmaceutically acceptable salt thereof; comprisingreacting the compound of formula (VIII-S) with carbon monoxide gas, wherein the carbon monoxide gas is present in an amount of about 60 psi; in the presence of a TEA, wherein the TEA is present in an amount of about 3.0 molar equivalents; in the presence of coupling system which is a 1:1 mixture of Pd(OAc)2 and XantPhos; wherein the Pd(OAc)2 is present in an amount of about 2.5 mol %; wherein the XantPhos is present in an amount of about 2.5 mol %; in an alcohol of the formula A1OH which is methanol or ethanol; at a temperature of about 80° C.