Stereoselective synthesis of new conformationally restricted analogues of a potent CGRP receptor antagonist |
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| Authors: | Zuev Dmitry Michne Jodi A Huang Hong Beno Brett R Wu Dedong Gao Qi Torrente John R Xu Cen Conway Charles M Macor John E Dubowchik Gene M |
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| Affiliation: | Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 5100, Wallingford, Connecticut 06492, USA. dmitry.zuev@bms.com |
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| Abstract: | [structures: see text] A stereocontrolled racemic synthesis of conformationally restricted analogues 2a and 2b of a potent CGRP receptor antagonist 1 by novel functionalization of 2-substituted octahydropyrido[1,2-a]pyrazin-6-ones is described. The new diastereoselective LDA-promoted alpha-nitration of intermediate lactams established the required trans-configuration in the desired products. |
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