Process for preparing 5-(R)-2-(5,6-diethylindan-2-ylamino)-1-hydroxyethyl-8-hydroxy-(1H)-quinolin-2-one (indacaterol)

摘要

The present invention relates to a novel process for the synthesis of 5 - [(R) -2- (5,6-diethylindan-2-ylamino) -1-hydroxyethyl] -8-hydroxy- (1H) -quinolin-2-one of formula (R) -2, known under the genetic name indacaterol, which is used to treat chronic obstructive pulmonary disease (COPD). The method comprises the preparation of a racemic intermediate 5- [2- (5,6-diethylindan-2-ylamino) -1-hydroxyethyl] -8-benzyloxy- (1H) -quinolin-2-one of formula 1, which in any order is chiral cleavage and debenzylate followed by isolation of indacaterol of formula (R) -2.