SYNTHESE DU FOSTEDIL (4-(2-BENZOTHIAZOLYL) BENZYLPHOSPHONATE DE DIETHYLE) A PARTIR D'IMIDATES N-ACYLES.

Fostedil (diethyl 4-(benzothiazol-2-yl) benzylphosphonate)7has been synthesized efficiently by treatment of 2-(4-bromomethylphenyl) benzothiazole6with triethylphosphite. The latter (6) has been prepared by bromation of benzothiazole3c. N-acylimidates1(a–d)react with 2-aminobenzenethiol2to lead to the corresponding benzothiazoles3(a–d)after elimination of primary amide5. The structure of these products have been unequivocally confirmed by means of IR,1H,13C, and31P NMR spectroscopy and mass spectra. [ABSTRACT FROM AUTHOR]