New Strategy for the Synthesis of Substituted Morpholines

摘要

A four-step synthesis of cis-3,5-disubstituted morpholines from enantiomerically pure amino alcohols is described.The key step in the synthesis is a Pd-catalyzed carboamination reaction between a substituted ethanolamine derivative and an aryl or alkenyl bromide.The morpholine products are generated as single stereoisomers in moderate to good yield.This strategy also provides access to fused bicyclic mor-pholines as well as 2,3-and 2,5-disubstituted products.