Back to Search Start Over

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

Authors :
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.
Source :
Organic Letters; June 2005, Vol. 7 Issue: 12 p2465-2468, 4p
Publication Year :
2005

Abstract

<UFIGR ID="ol0510062n00002">A stereocontrolled racemic synthesis of conformationally restricted analogues <BO>2a</BO> and <BO>2b</BO> of a potent CGRP receptor antagonist <BO>1</BO> 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.

Details

Language :
English
ISSN :
15237060 and 15237052
Volume :
7
Issue :
12
Database :
Supplemental Index
Journal :
Organic Letters
Publication Type :
Periodical
Accession number :
ejs7316805