Merck + Co., Inc.

Merck Frosst Canada, Inc.

Marck & Co., Inc.

Thomas R Verhoeven

Ichiro Shinkai

Robert D Larsen

Meyer Sletzinger

Chris H Senanayake

Andrew S Thompson

Ralph P Volante

F Edward Roberts

David M Tschaen

Kenneth M Ryan

James M McNamara

Ann E DeCamp

Dongwei Cai

Michel M Chartrain

Thomas M Liu

Anthony O King

Edward G Corley

Alan W Douglas

Steven A King

Lisa DiMichele

Neal C Connors

Mangzhu Zhao

Roger C Olewinski, Jr

Ann D Schuda

Robert N Young

Robert J Zamboni

Leonard M Weinstock

Paul J Reider

David Askin

Richard Frenette

Joseph F Payack

George M Garrity

Louis S Crocker

James A McCauley

Masatoshi Kakushima

David L Hughes

Robert A Reamer

Cheng Yi Chen

Richard Desmond

Gerald S Brenner

Jacques-Yves Gauthier

Yao-Jun Shi

Brian Heimbuch

Joseph D Armstrong, Iii

Karen C Thompson

Jinyou Zhang

Randolph L Greasham

Francis P Gailliot

Jennifer L Vandrilla

Barbara A Jackey

Sylvain Levac

Pamela M Simpson

Edward F Roberts

Ji Liu

Laura E Fredenburgh

Christ H Senanayake

Jennifer L Keller

Hossain Jahansouz

Chen Y Cheng

Chanyong Lee

Barry C Buckland

Meyer Sleteinger

A process of synthesizing a compound of the formula 1:

Process of synthesizing binaphthyl derivatives

A process is disclosed that bioconverts indene to (1S)-amino-(2R)-indanol substantially free of any of its stereoisomers, by the action of a strain of P. putida or Rhodococcus sp., followed by various chemical step(s), e.g., chiral specific crystallization, treatment with strong acid in the presence of acetonitrile.

Conversion of indene to (1S)-amino-(2R)-indanol free of any

The bisulfate salt of N,N-dimethyl-2-�5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl!ethylamine is a selective agonist of 5-HT.sub.1 -like receptors and is useful in the treatment of migraine and associated disorders.

Triazolylmethyl-indole ethylamine bisulfate salt

Polymorphic forms of the angiotensin II receptor antagonist, 3-�2'-(N-benzoyl)sulfonamidobiphenyl-4-yl!methyl-5,7-dimethyl-2-ethyl-3H-i midazo�4,5-b!pyridine and a method for the preparation of these crystal forms.

Polymorphic forms of an angiotensin II antagonist

The present invention relates to an improved process for the in situ preparation of diisopinocampheylchloroborane which comprises reacting sodium borohydride and boron trichloride with .alpha.-pinene. The diisopinocampheylchloroborane thus obtained may be used, without isolation, to reduce prochiral ketones to their corresponding alcohols in high optical purity.

Process for the preparation of diisopinocampheylchloroborane

A process is disclosed that quantitatively bioconverts indene to (1S,2R)-indene oxide and (1S,2R)-indandiol, by the action of fungal haloperoxidase followed by various chemical step(s), e.g., adjusting the pH.

Quantitative conversion of indene to (1S,2R) indene oxide and

.beta.- or .gamma.-Ketoesters and .beta.- or .gamma.-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40.degree. C. and about 50 N/mm.sup.2 of hydrogen in the presence of a strong acid.

Ruthenium-phosphine complex catalysts for asymmetric hydrogenations

A new process is described for the synthesis of the triazolyl tryptamine: ##STR1## and related compounds. The process involves a palladium-catalyzed ring closure between a substituted ortho-iodoaniline and a protected 1-alkynol. The process is carded out at high temperature, e.g. 100.degree. C., in a dry inert solvent, e.g., DMF and in the presence of a proton acceptor, e.g., Na.sub.2 CO.sub.3 or a trialkylamine. The triazolyl tryptamine, as well as acid addition salts thereof, is a 5 HT.sub.1 D receptor agonist having anti-migraine properties.

Palladium catalyzed ring closure of triazolyltryptamine

.beta.- or .gamma.-Ketoesters and .beta.- or .gamma.-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40.degree. C. and about 50N/mm.sup.2 of hydrogen in the presence of a strong acid.

Asymmetric hydrogenation of beta- or gamma-ketoesters and beta- or

A regioselective processes are disclosed for the synthesis of (1R,1S)-amino-(2S,2R)-alkanol, particularly (1R,1S)-amino-(2S,2R)-indanol.

Regiospecific processes to make cis-1-amino-2-alkanol from diol

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

Regiospecific processes to make CIS-1-Amino-2-Alkanol from Diol or

This invention relates to a method for the preparation of a compound of formula I: ##STR1## a key intermediate in the synthesis of a series of Angiotensin II receptor antagonists. The invention also relates to a selective reagent for conducting the Hofmann rearrangement, particularly in the formation of a pyridinoimidazolone, which is a percursor to the formation of an imidazopyfidine of formula I. This invention also relates to a method for the preparation of imidazolutidine, a key intermediate in the synthesis of 3-(2'-(N-benzoyl)sulfonamidobiphen-4-yl)-methyl-5,7 -dimethyl-2-ethyl-3H-imidazo[4,5-b]pyridine, using pyridinoimidazolone, an unreactive urea.

Process for the preparation of imidazolutidine

A regioselective process is disclosed for synthesis of 1R-amino-2S-indanol or 1S-amino-2R-indanol, wherein the stereochemical integrity of the carbon-oxygen bond at C-2 in the indene oxide starting material is retained.

Regiospecific process to make cis-1-amino-2-alkanol from epoxide

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Cranford, NJ, United States of America

Thomas R Verhoeven