Hovione Scientia Limited

Hovione Scienta Limited

Bruno Santos

Zita Mendes

Filipe Gaspar

Ana Carina Constantino

Constança Cacela

Celina Fernandes

Fernando Rocha

Pedro Valente

Paulo Ribeirinha

Adélio Mendes

A process for preparing (3R)-3-[2-Hydroxy(di-2-thienyl)acetoxy]-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide) comprises reacting 2-hydroxy-2,2-dithien-2-ylacetic acid 1-azabicyclo[2.2.2]oct-3(R) yl methyl ester and 3-phenoxypropyl bromide, wherein the reaction takes place in a solvent or mixture of solvents selected from the group of amides and/or the group of solvents with a sulfoxide group. Also provided is a crystalline aclidinium bromide characterized by a powder XRPD pattern having peaks at 7.7&#xb1;0.2&#xb0; 2&#x3b8;, 10.4&#xb1;0.2&#xb0; 2&#x3b8;, 13.2&#xb1;0.2&#xb0; 2&#x3b8;, 13.8&#xb1;0.2&#xb0; 2&#x3b8;, 19.9&#xb1;0.2&#xb0; 2&#x3b8;, 20.3&#xb1;0.2&#xb0; 2&#x3b8;, 20.8&#xb1;0.2&#xb0; 2&#x3b8;, 24.2&#xb1;0.2&#xb0; 2&#x3b8;, 25.7&#xb1;0.2&#xb0; 2&#x3b8;, 26.1&#xb1;0.2&#xb0; 2&#x3b8;, 29.2&#xb1;0.2&#xb0; 2&#x3b8;, 30.8&#xb1;0.2&#xb0; 2&#x3b8;. A pharmaceutical composition comprises aclidinium bromide according to the invention and a pharmaceutically acceptable excipient.

Process for the preparation of aclidinium bromide

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Odivelas, Portugal

Bruno Santos