Process for preparing scopine esters

US6747154B2 · kind B2 · utility

Assignee

• BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG · DE

Inventors

• Joerg Brandenburg · Ingelheim am Rhein, DE
• Waldemar Pfrengle · Seibersbach, DE
• Werner Rall · Mittelbiberach, DE

Key dates

• Filing date: Jan 9, 2003
• Grant date: Jun 8, 2004
• Expiry date: Jan 9, 2023

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P11/06
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A process for preparing a compound of formula 1 from a compound of formula 2 the process comprising reacting in one step the compound of formula 2 with a compound of formula 3 wherein:X− is chlorine, bromine, iodine, methanesulfonate, or trifluoromethanesulfonate;R1 is hydroxy, C1-C4-alkyl, C1-C4-alkoxy, CF3, or fluorine;Ar is phenyl, naphthyl, thienyl, and furyl, each optionally mono- or disubstituted with one or two groups selected from C1-C4-alkyl, C1-C4-alkoxy, hydroxy, fluorine, chlorine, bromine, or CF3;Y− is chlorine, bromine, iodine, methanesulfonate, or trifluoromethanesulfonate; andR is hydroxy, methoxy, ethoxy, O—N-succinimide, O—N-phthalimide, phenyloxy, nitrophenyloxy, fluorophenyloxy, pentafluorophenyloxy, vinyloxy, 2-allyloxy, —S-methyl, —S-ethyl, or —S-phenyl.