Merck + Co., Inc.

Degussa Aktiengesellschaft

Evonik Degussa Gmbh

Degussa Gmbh

Other

Kai Rossen

Ralph P Volante

Philip J Pye

Paul J Reider

David Askin

Robert D Larsen

Ian W Davies

Richard John Varsolona

Kenneth M Wells

Jess Sager

Steven A Weissman

Edward G Corley

Michel Journet

Linda Gerena

David J Mathre

Guo-Jie Ho

Roger N Farr

Martin Sarich

Ashok Maliakal

Karlheinz Drauz

Matthias Beller

Renat Kadyrov

Frank P Gortsema

Thomas Riermeier

Michael Schwarm

Peter Emmanuel Maligres

Louis S Crocker

Axel Monsees

Alexander Zapf

Daniel Richard Sidler

Oliver May

Juan Jose Almena Perea

Kan K Eng

Jonathan D Rosen

Milan Latinovic

Dieter Most

Harald Groeger

Carl LeBlond

Karel M Jos Brands

Veena Upadhyay

Shouichi Hiraga

Jean-Francois Marcoux

Daniel E Petrillo

Nobuya Satake

Todd D Nelson

Rolf Hoffmann

Stefan Eils

Wolf-Ruediger Krahnert

Stefan Klaus

Yongku Sun

Peter Gardner

Simon Rowell

The present invention is concerned with a process for preparing compounds of the general formula (I). These compounds can preferably be used to prepare bioactive agents. The reaction of the invention starts from the corresponding hydroxy compounds which are oxidized, with Ru catalysis, in a one-phase aqueous system. 

Process for preparing n-protected 4-ketoproline derivatives

A process for the preparation of an enantiomerically enriched amine, is performed by a) cleaving a racemic mixture of a reaction product of i) a chiral amine and ii) an acyl donor, in the presence of a hydrolase, to obtain a mixture of an enantiomerically enriched amide and an enantiomerically enriched amine; or b) reacting an amine with an acyl donor, in the presence of a hydrolase, to obtain a mixture of an enantiomerically enriched amide and an enantiomerically enriched amine; and c) separating the enantiomerically enriched amide from the enantiomerically enriched amine, wherein the acyl donor is a sulphonylacetic acid ester. The process (1) leads to high enantioselectivities, and (2) high reactivities, (3) is based on an acyl donor accessible in a simple manner, (4) is suitable for a large number of very different substrates and/or (5) is suitable for carrying out at high substrate concentrations.

Preparation of enantiomerically enriched amines and amides by enzymatic resolution using a sulfonylacetic acid ester as acyl donor

(Hetero)aromatic are prepared from halogen-substituted (hetero)aromatic compounds in the presence of a base and a palladium catalyst having a nonpyrophoric monodentate phosphane ligand. The phosphane ligand structure includes two radical groups having a tertiary carbon attached directly to phosphorous and one radical group having a primary carbon attached to the phosphorous.

Process for the preparation of aromatic aldehydes

The present invention is aimed at a process for the preparation of enantiomerically enriched compounds of general formula (I). These are obtained by classical resolution of the corresponding acid using a chiral amino base in organic solvents. 

Resolution of p-hydroxyphenyl-2-alkoxypropionic acids

5-formyl-2-furylboronic acid is produced by a) adding a base to a composition containing a boric acid ester and 2-furaldehyde, thereby obtaining a reaction mixture and protecting the formyl group of said 2-furaldehyde with a protective group, b) working-up of the reaction mixture in an acidic medium, and c) isolating of the 5-formyl-2-furylboronic acid.

Method of producing 5-formyl-2-furylboronic acid

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

The present invention is concerned with 4-benzyl-2-hydroxy-1,4-oxazin-3-one, and novel processes for the preparation therof. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.

4-Benzyl-2-hydroxy-1,4-oxazine-3-one and polymorphic forms thereof

Process for the preparation of hydroxylactones

The present invention is concerned with novel processes for the preparation of (2R-cis)-2-&lsqb;&lsqb;1-&lsqb;3.5-bis(trifluoromethyl)phenyl&rsqb;ethenyl&rsqb;oxy&rsqb;-3-(4-fluorophenyl)-4-(phenylmethyl) mopholine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.

Intramolecular 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

Process for the synthesis of carbapenem intermidiates, and compounds produced

The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Process for making diaryl pyridines useful as cox-2 inhibitors

Intermediates useful in a process for synthesizing COX-2 inhibitors

Process for making diaryl pyridines useful as COX-2 inhibitors

An improved process using chiral hydrogenation is described for the synthesis in high yields of a 4-protected-(S)-piperazine-2-tert-butylcarboxamide, an intermediate for an HIV protease inhibitor.

Process for preparing

The invention encompasses a process for making compounds of Formula I or Ia useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1##

Intermediates for making heterocycles useful as COX-2 inhibitors

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Westfield, NJ, United States of America

Kai Rossen