Preparation of chiral alpha-hydroxy-amides and carboxylic acids by controlled hydrolysis of corresponding hydroxynitriles with hydrochloric acid in carboxylic acid solvent

摘要

Method for preparing alpha -hydroxyamides or carboxylic acids (I) comprises reacting the corresponding hydroxynitrile (II) with hydrochloric acid in a 1-6C carboxylic acid solvent. Method for preparing alpha -hydroxyamides or carboxylic acids of formula (I) comprises reacting the corresponding hydroxynitrile of formula (II) with hydrochloric acid in a 1-6C carboxylic acid solvent, using either 25-37% HCl at 0-50 [deg] C to produce amides or 5-25% HCl at 20-100 [deg] C to produce acids. [Image] R1, R21-20C alkyl, 5-20C (hetero)aryl, 7-20C alkylaryl, 5-20C alkylheteroaryl or aralkyl, or 5-20C (alkyl)heterocycle (all optionally substituted once or multiple times); or R1+R2optionally substituted 4-20C alkylene optionally containing 1 or more heteroatoms; or one of R1 and R2 may : H; and X : NH2 or OH.