摘要

A new and versatile approach to prepare bicyclic lactams in moderate to high yield is reported herein. This approach, based on an extension of Meyers' method, provides 6,5-, 6,6- and 6,7-fused bicyclic lactams 6a-j from reaction of 1,8-naphthalaldehydic acid 7 with several aminoalcohols including L-serine, diamines and ethanethiol, in the absence of any catalyst. The reaction of 7 with (R)-phenylglycinol gave the 6,5-fused bicyclic lactam 6j in excellent diastereoselectivity (>98:2).

  • 出版日期2013