Patent ID: 7671199
Filing Date: 2010-03-02
Classification: A61P,C07D

Abstract:
1. A process for the preparation of Compound I of the formula comprising the steps of a) reacting Compound A of the formula with a methylating agent in a suitable solvent to afford Compound B of the formula b) which is reacted in a continuous oxidation followed by a quench reaction to prepare Compound C of the formula and protecting to convert Compound C to Compound D of the formula c) chlorinating Compound D to afford Compound E of the formula d) which is coupled with Compound F of the formula to afford Compound G of the formula, which is optionally crystallized to improve quality, and e) which is subsequently deprotected and reacted with (R)-(+)-propylene oxide in a suitable solvent, and optionally recrystallized to improve quality, to afford Compound H of the formula f) which is reacted with a Cbz-L-alanine and a coupling agent to afford Compound J of the formula g) which is deprotected and crystallized to afford crystalline Compound I.