Process for the preparation of...

C - Chemistry – Metallurgy – 07 – C

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C07C 209/74 (2006.01) C07C 213/08 (2006.01) C07F 9/165 (2006.01)

Patent

CA 2628098

The present invention relates to processes for the preparation of (.omega.- aminoalkylainino)alkyl halides, their conversion to S-.omega.-(.omega.- aminoalkylamino)alkyl phosphothioates, and purification of the crystalline products of the reaction. The preparation process for the (.omega.- aminoalkylamino)alkyl halides comprises contacting an appropriate alcohol with a brominating agent in the presence of a sulfone solvent under temperature and pressure conditions suitable to effect salt formation without subsequent premature precipitation. The process is especially useful for converting (.omega.-aminoalkylamino)ethyl alcohol to amifostine.

La présente invention concerne des procédés de fabrication d~halogénures de (.omega.- aminoalkylamino)alkyle, leur conversion en phosphothioates de S-.omega.-(.omega.-aminoalkylamino)alkyle et la purification des produits cristallins de la réaction. Le procédé de fabrication d~halogénures de (.omega.-aminoalkylamino)alkyle comprend la mise en contact d~un alcool approprié avec un agent bromant en présence d~un solvant sulfoné dans des conditions de température et de pression adaptées à la formation d~un sel sans précipitation prématurée subséquente. Le procédé est particulièrement utile pour la conversion d~alcool (.omega.-aminoalkylamino)éthylique en amifostine.

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