PROCESS FOR THE PREPARATION OF (ω -AMINOALKYLAMINO)ALKYL HALIDES AND CONVERSION TO AMIFOSTINE
The present invention relates to processes for the preparation of (ω- aminoalkylainino)alkyl halides, their conversion to S-ω-(ω-aminoalkylamino)alkyl phosphothioates, and purification of the crystalline products of the reaction. The preparation process for the (ω-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 (ω-aminoalkylamino)ethyl alcohol to amifostine.
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(2008/06/13)
CHIMIE DES RADIOPROTECTEURS: REVISION DE LA SYNTHESE DES ACIDES S- ET S-PHOSPHOROTHIOIQUES
Simple, reproducible and detailed preparations of S- and S- phosphorothioic acids (HO)2P(O)-S-(CH2)2-NH-(CH2)3-NH-R (R=H and CH3), named WR 2721 and WR 1680 respectively, are described.The yields of each step have been optimized to facilitate the synthesis of these compounds of large interest in the cancer radio- and chemotherapy.