A Convenient Synthesis of Substituted Pyrazolidines and Azaproline Derivatives through Highly Regio- and Diastereoselective Reduction of 2-Pyrazolines
作者:Jesús M. de los Santos、Yago López、Domitila Aparicio、Francisco Palacios
DOI:10.1021/jo702050t
日期:2008.1.1
The synthesis of substituted N-acetyl- and N-aroyl-2-pyrazolines via intramolecular Michael addition of α,β-unsaturated hydrazones generated through olefination of phosphinyl and phosphonyl hydrazones with carbonyl compounds is reported. The regioselective reduction of the C−N double bond in these 2-pyrazolines using Superhydride (Et3BHLi) gives pirazolidine derivatives with excellent levels of ci