Stereoselective Synthesis of New Conformationally Restricted Analogues of a Potent CGRP Receptor Antagonist

Autor: Zuev, D., Michne, J. A., Huang, H., Beno, B. R., Wu, D., Gao, Q., Torrente, J. R., Xu, C., Conway, C. M., Macor, J. E., Dubowchik, G. M.
Zdroj: Organic Letters; June 2005, Vol. 7 Issue: 12 p2465-2468, 4p
Abstrakt: 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 α-nitration of intermediate lactams established the required trans-configuration in the desired products.
Databáze: Supplemental Index