Merck + Co., Inc.

Richard Desmond

Sander G Mills

Ralph P Volante

Ichiro Shinkai

David M Tschaen

Todd K Jones

Ulf H Dolling

Richard D Tillyer

Thomas R Verhoeven

David Askin

Guo-Jie Ho

Robert A Reamer

Lisa F Frey

Dongwei Cai

Yao-Jun Shi

David Alan Conlon

Brenda Pipik

Anant Vailaya

Antoinette Drahus

Carl Leblond

Ben Marcune

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

Process for making substituted 8-arylquinolinium benzenesulfonate

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

Process of preparing phenyl heterocycles useful as COX-2 inhibitors

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

Process of making cox-2 inhibitors having a lactone bridge

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

A process is described for the total synthesis of the macrolide immunosuppressant, FK-506, and important tricarbonyl process intermediates thereof. The tricarbonyl intermediates can be produced by the mild oxidation of 2,3-dihydroxy carboxylate compounds containing olefin moieties.

Process for synthesis of FK-506 and tricarbonyl intermediates

A process is described for the improved synthesis of the optically pure C.sub.10 -C.sub.18 fragment of the macrolide structure of the immunosuppressant FK-506. This compound is also useful as an intermediate for preparing FK-506 derivatives.

FK-506 C10-C18 process intermediates

Process for synthesis of FK-506 C10-C18 intermediates

A process is described for the synthesis of E-2-methyl-.alpha.,.beta.-unsaturated aldehydes, which are useful as intermediates in the synthesis of the macrolide structure of the immunosuppressant FK-506. These compounds are also useful as ultraviolet radiation absorbers.

Process for synthesis of E-2-methyl-.alpha.,.beta.-unsaturated aldehydes

A process for producing arylglyoxal arylimine intermediates, by the DMSO/HBr oxidation of arylmethylketones. The imine compounds are intermediates in the synthesis of carbapenem antibiotics, i.e. imipenem.

Process for synthesis of arylglyoxal arylimines

The present invention is directed to an enantioselective synthesis of 1,3,4,6,7,12b(S)-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-one which is an intermediate in the production of the .alpha..sub.2 -adrenergic antagonist (2R,12bS)-N-(1,3,4,6,7,12-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-yl) -N-methyl-2-hydroxy-ethanesulfonamide hydrochloride.

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Bridgewater, NJ, United States of America

Richard Desmond