| 摘要 |
1,209,630. Benzoxazole and benzothiazole derivatives. CIBA Ltd. 28 Nov., 1967 [29 Nov., 1966; 19 Oct., 1967], No. 54084/67. Heading C2C. Novel benzoxazole and benzothiazole derivatives having a nucleus of the formula wherein X is an oxygen or sulphur atom, R is an esterified carboxyl or cyano group, R 2 is a carbo- C 1-4 alkoxy, cyano, or C 1-4 alkanoyl group, R 1 is a hydrogen atom or an aliphatic or cycloaliphatic hydrocarbon residue or an aryl group; and Ar is an at most bicyclic o-arylene radical which is optionally substituted by one or more C 1-4 alkyl, C 1-4 alkenyl, C 1-4 alkoxy, aryloxy, ar-C 1-4 - alkoxy, C 1-4 alkylthio, trifluoromethyl, nitro, free amino, C 1-4 alkylamino, di-C 1-4 -alkylamino, acylamino, carbamoylamino, thiocarbamoylamino, phenyl sulphonylamino, free sulpho, sulphamoyl, free or esterified carboxyl, cyano, carbamoyl, hydrazino-carbonyl, aryl, ar-C 1-4 - alkyl or C 1-4 alkylenedioxy groups or halogen atoms, and salts thereof are prepared by reaction of a benzoxazole or benzothiazole derivative of the general formula with a carbonyl compound of the general formula or with an enol derivative thereof, followed optionally by salt-formation. 2 - Amino - 4 - phenyl - benzothiazole and 2 - amino - 4 - trifluoromethyl - benzothiazole hydrobromide are prepared by reaction of N-(2- biphenylyl)-thiourea and N-(2-trifluoromethylphenyl)-thiourea, respectively, with bromine. 2 - Amino - 4 - (4 - chlorophenyloxy) - benzothiazole is prepared by reaction of 2-(4-chlorophenyloxy)-phenyl isothiocyanate with concentrated aqueous ammonia, followed by reaction of the resulting 2-(4-chloro-phenyloxy) - phenyl-thiourea with bromine. Pharmaceutical compositions having antifungal and antiviral activity comprise as active ingredient a novel benzoxazole or benzothiazole derivative as defined above and a pharmaceutically acceptable carrier.
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