Process for preparing substituted 3-(1-amino-2-methylpentane-3-yl)phenyl compounds

摘要

A process for the preparation of substituted 3-(1-amino-2-methylpentane-3-yl)phenyl compounds which has advantages over conventional processes with respect to higher conversions and yields, flexibility, a shorter overall route, environmentally acceptable conditions, influence of stereoselectivity such as diastereoselectivity in a targeted manner and at least partial suppression of the formation of undesired side-products and/or undesired stereoisomers, in particular undesired diastereomers.

主权项

1. A process for preparing a compound according to formula (I) wherein R1, R2 and R3 are each independently selected from the group consisting of H and C1-4-aliphatic residues, or a physiologically acceptable acid addition salt thereof, said process comprising the steps of: (b-I) converting a compound according to formula (B-I): into a compound according to formula (I), by reductive amination of said compound according to formula (B-I) to a compound according to formula (I) performed in the presence of an amine of formula H—NR1R2 and/or a salt thereof and at least one reducing agent,
wherein R1, R2 and R3 have the above defined meanings, and (b-II) optionally converting the compound according to formula (I) into a physiologically acceptable acid addition salt thereof.