Process for preparing a particular crystalline form of eletriptan hemisulphate

The present invention provides an improved process for the preparation of a polymorph of eletriptan hemisulphate. A process for preparing anhydrous eletriptan hemisulphate form I polymorph characterised by a powder X-ray diffraction pattern obtained using copper K-alpha1 radiation (lambda=0.15046 nm...

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Bibliographic Details
Main Authors DUNNE, CATHERINE, MACRAE, JULIE ANN, KLEINSCHROTH, JUERGEN FRIEDRICH, ARANDA-MARTINEZ, JULIAN, STOREY, RICHARD ANTHONY
Format Patent
LanguageEnglish
Published 11.12.2007
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:The present invention provides an improved process for the preparation of a polymorph of eletriptan hemisulphate. A process for preparing anhydrous eletriptan hemisulphate form I polymorph characterised by a powder X-ray diffraction pattern obtained using copper K-alpha1 radiation (lambda=0.15046 nm) which shows main peaks at 9.28, 10.38, 11.37, 12.40, 16.84, 17.46, 17.53, 17.78, 17.98, 19.48, 20.70, 21.29, 21.45, 22.21, 22.64, 23.08, 25.20 and 25.79, comprising the steps of (a) slurrying any other form of eletriptan hemisulphate in a solvent of the formula CH3COOR, wherein R is a C1-C6 alkyl group; (b) adjusting the water content of the slurry, if necessary, to 3% volume/volume or less; (c) heating the slurry; (d) concentrating the reaction mixture by azeotropic distillation, if necessary, until the water content of the reaction mixture has fallen to below 1% volume/volume; and (e) recovering the product.
Bibliography:Application Number: TW20040114789