Enantioselective acylation of aminoalkyl phenol comprises reacting an enantiomer mixture with acylating agent in the presence of hydrolase to obtain a mixture containing enantiomer in acylated and non-acylated forms

摘要

Enantioselective acylation of aminoalkyl phenol comprises reacting an enantiomeric mixture (II) with an acylating agent in the presence of a hydrolase to obtain a mixture containing enantiomers, preferably in acylated and non-acylated forms. Enantioselective acylation of aminoalkyl phenol comprises reacting an enantiomeric mixture of formula (II) with an acylating agent in the presence of a hydrolase to obtain a mixture containing enantiomers, preferably in acylated and in non-acylated forms. P : a protective group; and m, n : 0-2. An independent claim is also included for preparation of an optically active enantiomeric mixture (II) (in R and/or S enantiomeric form), which comprises: (a) reacting (II) with an acylating agent in the presence of a hydrolase to obtain a mixture that contains an enantiomeric mixture containing enantiomers in acylated and non-acylated forms; (b) separating the acylated enantiomers from the mixture; (c) deprotecting the non-acylated enantiomers to obtain an amine in S or R enantiomeric form; and (d) hydrolyzing the acylated enantiomers to its corresponding non-acylated enantiomers of the amines and subsequent deprotection to give amine in R or S enantiomeric form. [Image].