Process for the preparation of optically pure fesoterodine derivatives

US9422228B2 · kind B2 · utility

Assignee

• CRYSTAL PHARMA, S.A.U. · ES

Inventors

• Antonio Lorente Bonde-Larsen · Laguna de Duero, ES
• Francisco Javier Gallo Nieto · Laguna de Duero, ES
• Juan José Ferreiro Gil · Laguna de Duero, ES
• Pablo Martín Pascual · Laguna de Duero, ES

Key dates

• Filing date: Apr 26, 2013
• Grant date: Aug 23, 2016
• Expiry date: Apr 26, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

3,3-diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, can be produced by treating a compound of formula (II) with a chiral alcohol to yield the diastereomeric esters of formula (IV) and (IV′), which can be further transformed into a compound of formula (I), or an enantiomer, solvate or salt thereof, wherein R1 is C1-C8 alkyl; and R2 and R3, independently of one another, represent H or C1-C6 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound.