PROCESS FOR THE PREPARATION OF (? -AMINOALKYLAMINO)ALKYL HALIDES AND CONVERSION TO AMIFOSTINE

摘要

The present invention relates to processes for the preparation of (?- aminoalkylainino)alkyl halides, their conversion to S-?-(?-aminoalkylamino)alkyl phosphothioates, and purification of the crystalline products of the reaction. The preparation process for the (?-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 (?-aminoalkylamino)ethyl alcohol to amifostine.