Merck + Co., Inc.

Solvias Ag

Yongkui Sun

Thorsten Rosner

Yi Xiao

Nelo R Rivera

Joseph D Armstrong, Iii

Shane W Krska

Carl LeBlond

Felix Spindler

Paul J Reider

Mark A Huffman

Christophe Malan

Eugenia Njolito

John R Sowa, Jr

Andrew M Clausen

The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.

Process for the preparation of enantiomerically enriched beta amino acid derivatives

The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.

Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation

Iodohydroxylated olefins can be prepared by treating an olefin with an aqueous solution of an iodine monohalide selected from iodine monochloride and iodine monobromide.

Iodohydroxylation of olefins

The present invention relates to a process wherein heterogeneous finely-dispersed palladium catalysts are used in a cross-coupling reaction of alkenyl halides and aryl or heteroaryl boronic acids in the presence of base in an aprotic solvent to produce aryl- or heteroaryl-olefin compounds of Formula I:

Heterogeneously catalyzed process for cross coupling alkenyl halides with boronic acids

The invention relates to an improved stereoselective heterogenous catalytic reductive amination between ethyl 2-oxo-4-phenylbutyrate and alanylproline using hydrogen, a catalyst and one or more additives to produce the ACE inhibitor, enalapril.

Stereoselective process for enalapril

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Bridgewater, NJ, United States of America

Yongkui Sun