Merck + Co., Inc.

Horizon Therapeutics, LLC

Merck Sharp + Dohme Corp.

Banyu Pharmaceutical Co. Ltd

Concert Pharmaceuticals, Inc.

Other

Msd K.k.

Steven A Weissman

Ralph P Volante

Andrew S Thompson

Kai Rossen

David M Tschaen

David Askin

Steven S Pfeiffer

Takehiko Iida

Huai-Chueh Chang

Vasilios H Iskos

Maki Uragami

Kenji Maeda

Paul J Reider

Peter Emmanuel Maligres

Ramanaiah C Kanamarlapudi

Emerich Eisenreich

Xuejun Karl Liu

Shouichi Hiraga

Kenichi Asakawa

Hiroki Sato

Matthew Heileman

Nobuya Satake

Makoto Ishikawa

Masashi Kawasaki

Guy R Humphrey

Robert D Larsen

Toshiaki Mase

Nobuaki Nonoyama

Shinji Kato

Ross A Miller

Yuji Haga

Daniel Richard Sidler

Joseph Auerbach

Robert Wenslow

Yaling Wang

Kan K Eng

Nancy Sue Barta

Aaron J Moment

Russell R Ferlita

Jess Sager

Veena Upadhyay

Daniel E Petrillo

Asayuki Kamatani

Hisaki Kojima

Robert M Wenslow

Kazuki Shigemori

Stephanie Lewis

Keisuke Kamei

Provided is a process for preparing 4-phenyl-1-butyric acid, comprising: reacting 4-phenyl-1-butanol with sodium chlorite, a nitroxyl radical catalyst and sodium hypochlorite in an organic solvent and a phosphate buffer; and quenching the reaction with sodium sulfite to produce 4-phenyl-1-butyric. Also provided is 4-phenyl-1-butyric acid prepared by such a process.

Procedure for the preparation of 4-phenyl butyrate and uses thereof

The present invention provides a convenient and efficient process for the preparation of enantiomerically enriched, deuterated secondary alcohols without reducing deuterium incorporation.

Process for preparing an enantiomerically enriched, deuterated secondary alcohol from a corresponding ketone without reducing deuterium incorporation

The present invention provides a process for the preparation of enantiomerically enriched, deuterated secondary alcohols of Formula 1-A by employing ketoreductases or carbonyl reductases without reducing deuterium incorporation. 

Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)-2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed. 

Process for preparing N-substituted hydroxypyrimidinone carboxamides

The present invention relates to a process for producing crystalline trans-N-[1-(2-fluorophenyl)-S-pyrazoly]-3-ox-ospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4&#x2032;-carboxamide and novel salts, hydrates and polymorphs thereof.

Synthesis and crystalline forms of NPY5 antagonist

A practical, ligand-free cyanation of aryl bromides employs Pd catalyst in combination with a non-toxic cyanide source, M[Fe(CN)] (M=K or Na; n is 3 or 4), or a hydrate thereof, and a base. The reactions are performed in a polar aprotic solvents and provide the corresponding aryl nitrile in 83-96% yield, typically in less than 5 h.

Cyanation of aromatic halides

This invention relates to a process for making spirolactone compounds analogous to formula I. 

Process for making spirolactone compounds

This invention relates to a process for making spirolactone compounds analogous to formula I 

The present invention relates to a novel process to make indolocarbazole glycosides in high purity which inhibit the growth of tumor cells and are therefore useful in the treatment of cancer in mammals, and the like.

Preparation and isolation of indolocarbazole glycosides

The present invention relates to a novel glycosidation process to make intermediates useful in the preparation of indolopyrrolocarbazole derivatives which inhibit the growth of tumor cells and are therefore useful in the treatment of cancer in mammals, and the like.

Phase transfer catalyzed glycosidation of an indolocarbazole

A process for preparing a &bgr;-hydroxy carbamate product is disclosed. The process comprises reacting an olefin compound containing at least one carbon-carbon double bond with a carbamate in an aqueous solvent and in the presence of a base, an osmium catalyst, a co-oxidant selected from a halohydantoin, a haloisocyanuric acid, and an alkali metal salt of a haloisocyanuric acid, and optionally an asymmetric ligand, to form a reaction mixture containing the &bgr;-hydroxy carbamate product. The process optionally further comprises treating the &bgr;-hydroxy carbamate product with additional base to form an oxazolidinone. The oxazolidinones are useful as chiral auxiliary agents and as intermediates for the formation of pharmaceutically active substances such as alpha 1 a adrenergic receptor antagonists. A process for preparing nitrogen-functionalized derivatives of the oxazolidinones is also disclosed.

Process for preparing &bgr;-hydroxycarbamates and their conversion to oxazolidinones

The present invention is directed to a process for synthesizing substituted piperazinones, which are useful intermediates for making farnesyl-protein transferase inhibitors, using a Mitsunobu reaction.

Process for the synthesis of substituted piperazinones via Mitsunobu

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

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Little Falls, NJ, United States of America

Steven A Weissman