Merck + Co., Inc.

Julie J Mohan

Edward J Grabowski

David J Mathre

Thomas J Blacklock

Paul Sohar

Todd K Jones

Lyndon C Xavier

F Edward Roberts

5,6-Dihydro-4-(R-amino)-4H-thieno[2,3-b]-thiopyran-2-sulfonamide-7,7-dioxid e is a potent carbonic anhydrase inhibitor useful in the treatment of ocular hypertension and glaucoma. The S-(+)-enantiomer of that compound, the more active enantiomer, is prepared by a process involving an intermediate step of an enantioselective reduction of a carbonyl group employing an oxazaborolidine chiral catalyst.

Enantiospecific synthesis of

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Edison, NJ, United States of America

Julie J Mohan