Merck + Co., Inc.

Other

David Alan Conlon

Guo-Jie Ho

Brenda Pipik

Antoinette Drahus

Anant Vailaya

Nobuyoshi Yasuda

Barry M Trost

Richard Desmond

Dwight Macdonald

Sophie-Dorothee Clas

Michael Palucki

Steven A King

Paul Compton Collins

Christopher Joseph Welch

Joann M Um

Mirlinda Biba

Carl Leblond

Roch Thibert

Helene Perrier

Elizabeth Kwong

A purification method in the preparation of a substituted 8-arylquinoline, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, utilizes a polystyrene-based sulfonylhydrazine reactive resin to remove an aldehyde impurity.

Removal of aldehyde impurity by reactive polystyrene resini

A substituted 8-aryl quinoline and its benzenesulfonic acid salt is synthesized.

Process for making substituted 8-arylquinolinium benzenesulfonate

Novel sulfuric acid, methanesulfonic acid, p-toluenesulfonic acid, 2-naphthalenesulfonic acid, hydrochloride acid, or benzenesulfonic acid salts of substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.

Substituted 8-arylquinoline phosphodiesterase-4 inhibitors

Processes are disclosed for preparing 3-hydroxymethylcyclopentanone compounds, which are useful as intermediates in the preparation of HIV chemokine CCR-5 receptor antagonists. A process is described in which the compounds are prepared by opening the cyclopropyl ring of a (1-alkoxycarbonyl-2-oxo)-trans-bicyclo&lsqb;3.1.0&rsqb;hexane compound by addition of a nucleophile to the cyclopropyl ring, and then decarboxylating the resulting 2-alkoxycarbonyl-3-(Nu-methyl)-cyclopentanone (Nu&equals;the added nucleophilic group) via base solvolysis. Also described is a process for preparing the bicyclo&lsqb;3.1.0&rsqb;hexane precursors by the catalyzed cyclopropanation of a suitable alpha-diazo-beta-ketoester. The preparation of the alpha-diazo-beta-ketoesters and precursors thereto are also disclosed.

Process for preparing 3-hydroxymethyl-4-(aryl or heterocyclic)-cyclopentanones

The present invention provides a novel process for the preparation of 1,1-cyclopropanedimethanol cyclic sulfite which comprises: (a) contacting 1,1-cyclopropanedimethanol with dialkylsulfite in the presence of a base; and (b) removing from the reaction mixture the alcohol reaction by-product. This process is incorporated in the additional novel processes for preparing 1-(hydroxymethyl)cyclopropaneacetonitrile and 1-(thiomethyl)cyclopropaneacetic acid.

Process for the preparation of 1-(thiomethyl)-cyclopropaneacetic acid

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Plainsboro, NJ, United States of America

David Alan Conlon