PROCESS FOR PREPARING GUANIDINO-THIAZOLE COMPOUNDS

摘要

Guanidinothiazoles I [ R=H, alky1; Y=S, methylene; m,n=1˜3; A=C(:NR1)NHR2, -CONF-R4; R1=H, cyano, CONH2, ureido, OH, alkoxy, acy1, acy1amino, aryisulfamoy1, aralky1, CH2CO2H, alkylsulfony1, arylsulfony1; R2=H, aliph., cyano, acy1; R4=H, alky1, OH, SO2NH2 were prepd. Thus, A (R=H; m=1; Y=S; n=2; X=NCN; R'=NH2) was obtained by ethanolysis of the methylthio-propionitrile and treatment of the propionimidate with H2NCN. A had a histaminic H2 receptor blocking ED50 of 18.3 μg/kg i.v. in rats.