A practical synthesis for the core structure of a family of selective prostaglandin D2 receptor antagonists |
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| Authors: | Campos Kevin R Journet Michel Cai Dongwei Kowal Jason J Lee Sandra Larsen Robert D Reider Paul J |
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| Affiliation: | Department of Process Research, Merck Research Laboratories, P.O. Box, 2000, RY800-B267, Rahway, New Jersey 07065-0900, USA. kevin_campos@merck.com |
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| Abstract: | A convergent synthesis was developed for the production of the core structure of prostaglandin D(2) receptor antagonists for the treatment of allergic rhinitis. The key steps in this synthesis were a highly diastereoselective alkylation of (+)-nopinone, a chemo- and stereoselective reduction of an oxime to an amine, and a well-controlled reduction of an aminoalkyne to a (Z)-olefin. |
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