Merck + Co., Inc.

Roger N Farr

Ralph P Volante

Kai Rossen

David J Mathre

Guo-Jie Ho

Guy R Humphrey

John Y L Chung

Process for the synthesis of gonadotropin releasing hormone antagonists

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

Intermediates for making heterocycles useful as COX-2 inhibitors

Disclosed are compounds of the formula: ##STR1## where R is selected from the group consisting of C.sub.1 -C.sub.4 linear or branched alkyl, trifluoromethyl, halo, phenyl, biphenyl and naphthyl, wherein the aromatic group can be substituted with C.sub.1 -C.sub.4 linear or branched alkyl, trifluoromethyl, or halo; and wherein the asterisked 3-position ring carbon is either in (R) or (S) configuration, or racemate form, and salts thereof formula I. The compounds are useful in chiral synthesis, for example, producing naturally occurring L-amino acids, e.g., alanine, from aliphatic acid precursors.

3-substitutes isoxazolidines as chiral auxiliary agents

Process for making phenyl heterocycles useful as cox-2 inhibitors

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Whitehouse Station, NJ, United States of America

Roger N Farr