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
Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 5100, Wallingford, Connecticut 06492, USA.
Org Lett. 2005 Jun 9;7(12):2465-8. doi: 10.1021/ol0510062.
[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.
[结构：见正文] 描述了通过对2-取代八氢吡啶并[1,2-a]吡嗪-6-酮进行新型官能团化，对强效降钙素基因相关肽（CGRP）受体拮抗剂1的构象受限类似物2a和2b进行立体控制的外消旋合成。中间体内酰胺的新型非对映选择性LDA促进的α-硝化反应在所需产物中建立了所需的反式构型。
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