Merck + Co., Inc.

Merck Sharp + Dohme Corp.

James M McNamara

Ralph P Volante

Thomas R Verhoeven

Meyer Sletzinger

Thomas M Liu

Edward G Corley

Daniel Richard Sidler

Jonathan D Rosen

Louis Matty

James J Bergan

Mahadevan Bhupathy

Paul J Reider

Michel M Chartrain

Dalian Zhao

Joseph S Amato

Matthew Mangzhu Zhao

David L Hughes

John Y Chung

Robert A Reamer

Johnnie L Leazer, Jr

The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl) -morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.

Process for {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid

The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(tri-fluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.

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The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R, 3a)-2-&lsqb;1-&lsqb;3,5-bis(trifluoromethyl)phenyl&rsqb;ethoxy-3-(4-fluorophenyl)-1,4-oxazine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.

Trans-glycosidation process for the synthesis of (2R, 2-alpha-R, 3a)-2-&lsqb;1-(3,5-bis(trifluoromethyl)phenyl)ethoxy&rsqb;-3-(4-fluorophenyl)-1,4-oxazine

The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof

Process for the preparation of leukotriene antagonists

A bioconversion process where benzyl acetoacetate is converted to benzyl-(S)-(+)-3-hydroxybutyrate.

Stereospecific bioconversion of benzyl acetoacetate to

Pyridyl ethylation of lactams

The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof ##STR1## wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercaptomethyl)cyclopropaneacetic acid with a compound of formula (II) ##STR2## wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I).

Process for the preparation of leukotriene anatgonists

This invention relates to a novel process for preparing unsymmetrical dithioacetals and dithioketals from aryl aldehydes and ketones.

Process for unsymmetrical dithioacetals and dithioketals

A stereoselective process for the preparation of antihypercholesterolemic agents of the HMG-CoA reductase inhibitor type comprises treatment of an intermediate .beta.-hydroxyketone with a trialkylborane and sodium borohydride at low temperatures.

Process for preparing HMG-CoA reductase inhibitors with a

This invention relates to a novel process for the preparation of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which contain a 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety, such as compactin and mevinolin, by utilizing an alkyl 4-cyano-3(R)-hydroxybutanoate as a chiral synthon for the stereospecific introduction of the 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety.

Process for the preparation of HMG-CoA reductase inhibitors and

This invention relates to a novel process for the preparation of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which contain a 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety, such as compactin and mevinolin, by utilizing an alkyl 4-halo-3(S)-hydroxybutanoate as a chiral synthon for the stereospecific introduction of the 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety.

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Rahway, NJ, United States of America

James M McNamara