Merck + Co., Inc.

Yao-Jun Shi

Joseph E Lynch

Kenneth M Wells

David R Lieberman

Michael A Robbins

Thomas R Verhoeven

David M Tschaen

Richard Desmond

Dongwei Cai

Michael J Kaufman

Mark Cameron

Shyam B Karki

&Ouml;rn Almarsson

Maneesh J Nerurkar

Process for the preparation of conjugates useful in the treatment of prostate cancer

Salt form of a conjugate useful in the treatment of prostate cancer

The present invention is directed to an improved process for preparing the phenylacetic acid side chain of the compound of the formula ##STR1## This compound exhibits utility as a Class III antiarrhythmic agent.

Side chains synthesis for an anthiarrhythmic compound

The invention encompasses a novel process for the formation of enantiomerically enriched mixtures of compounds of Formula I, which are useful precursors in the synthesis of phosphodiestersae IV inhibitors.

Process for phosphodiesterase IV inhibitors

The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.

Process for regioselective substitution of trifluorobenzoate or

The present invention is directed to a process of making spirocycles of general structural formula: ##STR1## where R.sub.1 is selected from the group consisting of CO--C.sub.1-3 alkyl, cyano, carboxy, carboxy C.sub.1-6 alkyl ester, carboxamide, C.sub.1-6 alkyl sulfinyl, C.sub.1-6 alkyl sulfonyl, C.sub.1-6 methanesulfonamide and halogen; R.sub.2 is selected from the group consisting of keto or alcohol, R.sub.3 is cyano, resulting in compounds which are Class III antiarrhythmic.

Process of making spirocycles and analogs thereof

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Edison, NJ, United States of America

Yao-Jun Shi