APPLICATION OF CHIRAL AMINOPHENOL LIGAND IN ASYMMETRIC SYNTHESIS OF EFAVIRENZ

摘要

The present invention relates to an application of a chiral aminophenol ligand in asymmetric synthesis of efavirenz. A chiral aminophenol ligand compound is used for inducing asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-1,3-benzoxazine-2-ketone (efavirenz). The ligand is cheap, easily available, safe and recoverable, is used in asymmetric synthesis of efavirenz, and has the advantages of high yield, good enantioselectivity, simplicity and convenience in operation, capability of realizing industrialized production and good product quality.