NOVEL 2-AMINO-1,3,4-THIADIAZOLE DERIVATIVE

摘要

NEW MATERIAL:A compound of formulaI(R is H or a group of formula II; n is 0 or 1) and an acid addition salt thereof. EXAMPLE:2-(alpha-2-Thienylglycyl)amino-1,3,4-thiadiazole hydrochloride. USE:An antitumor agent exhibiting improved activity particularly against malignant tumors, e.g. leukemia, sarcoma, cancer, etc. PROCESS:An amino acid of formula II or a reactive derivative, e.g. an acid chloride, azide or phenyl ester, is reacted with a 2-amino-1,3,4-thiadiazole of formula IV or a reactive derivative, e.g. an isocyanate or phosphazo compound, in the presence of a dehydrating agent, e.g. N,N'-dicyclohexylcarbodiimide, or a condensing agent, e.g. a chlorocarbonic ester, at -70-+250 deg.C for 1-30hr to give the aimed compound of formulaI.