New Synthetic Pathway To Diverse 2-Substituted Quinolines Based on a Multicomponent Reaction:Solution-Phase and Solid-Phase Applications

摘要

Using Kobayashi's modification of the Grieco reaction,we were able to synthesize diverse 4-phenylthio-1,2,3,4-tetrahydroquinolines.These intermediates were oxidized and subsequently pyrolized to provide the corresponding quinolines.This new approach to 2-substituted quinolines was exemplified by liquid-phase production of a 25-member library.This was extended to solid-phase chemistry,starting from (L)-4-nitrophenylalanine on Wang resin,for production of a 16-member library.The latter compounds possess potentially interesting VLA-4 antagonist properties.