| 摘要 |
<p>1410787 3-Arylsulphonyl-1,2,4-oxadiazoles E R SQUIBB & SONS Inc 3 Oct 1972 [19 Oct 1971] 45615/72 Heading C2C Novel 3-arylsulphonyl-1,2,4-oxadiazoles of Formula I wherein R is H, -CCl 3 , -NH 2 , C 1 -C 8 alkylamino, guanidino, -OH, C 1 -C 8 alkoxy or C 1 -C 8 alkylthio; R 1 is H, C 1 -C 8 alkyl, NH 2 , C 1 -C 8 alkylamino, C 1 -C 8 alkanoylamino, halogen, -NO 2 , -CO 2 H, or C 1 -C 8 alkyl-O.CO- and n is 1, 2 or 3 together with acid addition salts thereof may be prepared by heating a compound of Formula IV in order to cause cyclization or by cyclizing a compound of Formula IV wherein R is -CCl 3 to form the corresponding compound of Formula I in which R is -CCl 3 and reacting this product with a compound RH wherein R is -NH 2 , C 1 -C 8 alkylamino, guanidino, -OH, C 1 -C 8 alkoxy or C 1 -C 8 alkylthio and if required treating such a compound to form its acid addition salts. Phenyl sulphonylformamidoximes are prepared by reacting the corresponding phenyl. sulphonylcyanide with hydroxylamine or a salt thereof and in examples R 1 is H, Cl, CH 3 , CH 3 CONH. These compounds may be reacted with an acid anhydride, acid halide or mixed acid ester halide to give compounds of Formula IV (above). In examples of such intermediates R 1 is H and R is CH 2 Cl, -CH 2 -CH 2 CO 2 H, -CH 2 CH 2 CO 2 CH 3 , -(CH 2 ) 4 Cl, -CCl 3 , and N.PL. Pharmaceutical compositions of the compounds I optionally together with conventional excipients show antimicrobial and hypoglycemic activity when administered orally, topically or parenterally in capsule, tablet, elixir, injection, lotion, salve or cream form. Disinfectant compositions of the compounds I may also comprise inert solids or liquids i.e. in dusts or sprays, soaps, solid or liquid detergents or detergent compositions.</p> |
