Merck + Co., Inc.

Marck & Co., Inc.

Chris H Senanayake

Thomas R Verhoeven

Robert D Larsen

Michel M Chartrain

Kenneth M Ryan

F Edward Roberts

Dhileepkumar Krishnamurthy

Zhengxu Han

Wenjun Tang

Xiufeng Sun

Xiao-Jun Wang

Frank Himmelsbach

Matthias Eckhardt

Andrew S Thompson

Sheo B Singh

Paul J Reider

Louis S Crocker

Robert A Reamer

John P Rosazza

Gerald S Brenner

Jason Alan Mulder

Brian Heimbuch

Karen C Thompson

Jinyou Zhang

Randolph L Greasham

Neal C Connors

Roger C Olewinski, Jr

Barbara A Jackey

Francis P Gailliot

Hossain Jahansouz

Laura E Fredenburgh

Barry C Buckland

Chanyong Lee

Timothy Bill

Thomas R Vernhoeven

Edward F Roberts

Ji Liu

Thomas G Tampone

Xudong Wei

Nitinchandra Patel

Pascale Aj Pouzet

Peter Nickolaus

Ulrike Werthmann

Rogelio P Frutos

Bing-Shiou Yang

Soojin Kim

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

A process is disclosed that hydrolyzes, by the action of an epoxide hydrolase of Diplodia gossipina (alternatively named Diplodia gossypina) ATCC 16391 or ATCC 10936, the undesired enantiomer of racemic indene oxide, an epoxide of indan.

Resolution of racemic indene oxide to yield (1S,2R)-indene oxide using

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

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

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

The natural stereochemistry at the 13-position of avermectin aglycones, normally .alpha.-oriented or below the plane of the molecule, is inverted or epimerized into the .beta.-position. The procedure starts with the avermectin aglycone compounds where the 13.alpha.-hydroxy group is activated to a mesylate leaving group. The resultant 13-.alpha.-mesylate is then displaced with a cesium carboxylate and one equivalent of the respective carboxylic acid, ending with the ester group being converted to the 13-.beta.-hydroxy configuration by transesterification in high yield.

Process for converting the 13-.alpha.-hydroxy group of avermectin

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North Brunswick, NJ, United States of America

Chris H Senanayake