VERFAHREN ZUR DIASTEREOSELEKTIVEN REDUKTION VON 3-AMINO-1-BENZOXEPIN-5(2H)-ONEN

摘要

A process for producing cis-2,3,4,5-tetrahydro-3-amino-1-benzoxepin-5-ols in which 3-amino-1-benzoxepin-5(2H)-ones are diastereoselectively reduced in a single stage by catalytic hydrogenation in the presence of a platinum oxide catalyst and an equivalent amount of an acid in a polar protic solvent, or by reaction with a borane/amine complex in an aprotic solvent, optionally in the presence of an added lower aliphatic carboxylic acid.