Process for obtaining olopatadine and intermediates

US9000195B2 · kind B2 · utility

Assignee

• CRYSTAL PHARMA, S.A.U. · ES

Inventors

• Luis Octavio Silva Guisasola · Boecillo, ES
• Lydia Mateos Burón · Laguna de Duero, ES
• Antonio Lorente Bonde-Larsen · Laguna de Duero, ES
• Luis Gerardo Gutiérrez Fuentes · Laguna de Duero, ES

Key dates

• Filing date: Jul 14, 2009
• Grant date: Apr 7, 2015
• Expiry date: Dec 22, 2030

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Olopatadine can be obtained by means of a process comprising hydrolysis of a compound of general formula (II), wherein Y is OR1, wherein R1 is C1-C7 alkyl, C3-C7 cycloalkyl, aryl, arylalkyl, or heterocycle; or NR2R3, wherein R2 and R3, independently from each other, are C1-C7 alkyl, aryl, arylalkyl, or R2 and R3 together with the nitrogen atom to which they are bound form a heterocycle of 3 to 7 members, obtained by means of a process comprising reacting the corresponding ester or amide of 6,11-dihydro-11-oxodibenz[b,e]oxepin-2-acetic acid with a suitable Wittig reagent, in the presence of a base in a reaction medium comprising an organic solvent.