Merck + Co., Inc.

Kan K Eng

Ralph P Volante

David Askin

Paul J Reider

Kai Rossen

Peter Emmanuel Maligres

Steven A Weissman

Ioannis N Houpis

Ilias K Dorziotis

Veena Upadhyay

The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1##

Process for making phenyl heterocycles useful as COX-2 inhibitors

A process for synthesizing the epoxide of the formula ##STR1## consists of, at a minimum, formation of a halohydrin from the allyl acetonide reactat, followed by base-induced cyclization, the epoxide product I being useful as an intermediate for the synthesis of inhibitors of renin or HIV protease or other proteases.

Process for making an epoxide

A process for making a clinically efficacious HIV protease inhibitor eliminates one step in its synthesis, by an alternative convergent synthesis using 2(S)-4-picolyl-2-piperazine-t-butylcarboxamide as an intermediate.

Process to make HIV protease inhibitor from

Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.

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Jersey City, NJ, United States of America

Kan K Eng