| 摘要 |
<p>1,178,786. 5 - Benzylamino - 1,3,4 - oxathiazole - 3,3 - dioxides. FARBENFABRIKEN BAYER A.G. 5 July, 1968 [6 July, 1967], No. 32264/68. Heading C2C. Novel 5 - benzylamino - 1,3,4 - oxathiazole- 3,3-dioxides of the general formula wherein R<SP>1</SP> is a hydrogen atom or a methyl group; R<SP>2</SP> and R<SP>3</SP> are each a hydrogen atom, a C 1-4 alkyl group, a di-alkylarnino-C 2-5 alkyl group with a total of 2 to 8 carbon atoms in the N-alkyl groups or a dialkylamino-C 2-5 alkyl group in which the two alkyl groups contain a total of 4-8 carbon atoms and are linked via an O or S atom or a CH 2 , NH or SO 2 group to form a heterocyclic ring; R<SP>4</SP> is a hydrogen or halogen atom or a C 1-4 alkyl group; and R<SP>5</SP> is a hydrogen, or halogen atom, a C 1-4 alkyl, nitro or trifluoromethyl group, a dialkylamino group with a total of 2-8 carbon atoms, a dialkylamino group with a total of 4-8 carbon atoms, the alkyl groups of which are linked via an O or S atom or a CH 2 , NH or SO 2 group to form a heterocyclic ring, a di-alkylamino-C 2-5 alkyl group with a total of 2 to 8 carbon atoms in the N-alkyl groups or a di-alkylamino-C 2-5 alkyl group in which the two alkyl groups contain a total of 4-8 carbon atoms and are linked via an O or atom or a CH 2 , NH or SO 2 group to form a heterocyclic ring; and salts thereof with organic or inorganic acids or bases are prepared (a) by cyclization of an N-x-haloalkane-sulphonyl-N<SP>1</SP>-benzyl-urea of the general formula wherein X is a chlorine, bromine or iodine atom in the presence of at least the stoichiometric amount of an alkali metal hydroxide or alkaline earth metal hydroxide or tertiary organic base in a polar organic solvent at a temperature of from 30‹ to 150‹ C.: (b) by reaction of an N-(α- haloalkane-sulphonyl)-arylcarbamate of the general formula X-CHR<SP>1</SP>-SO 2 NH-COOAr, wherein Ar is an optionally substituted aromatic radical, with a benzylamine of the general formula followed by cyclization in the presence of at least the stoichiometric amount of an alkali metal hydroxide or an alkaline earth metal hydroxide or a tertiary organic base in a polar organic solvent at a temperature of from 30‹ to 150‹ C., or (c) by reaction of. a 5-amino-1,3,4- oxathiazole-3,3-dioxide of the general formula with a benzyl halide of the general formula followed optionally by salification of the product. N - Chloromethanesulphonyl - phenylcarbamate is prepared by reaction of chloromethanesulphonamide with phenyl chloroformate. N-α- Chloroethanesulphonyl - N<SP>1</SP> -3 - chlorobenzylurea is prepared by reaction ofα-chloroethanesulphochloride with ammonia, followed by reaction of the resultingα-chloroethane-sulphonamide with 3-chlorobenzyl isocyanate. Pharmaceutical compositions having tranquillizing and ataraxic properties comprise, as active ingredient, a 5-benzylamino-1,3,4-oxathiazole-3,3-dioxide of the first general formula above or a salt thereof with a physiologically acceptable, non-toxic, inorganic or-organic acid or base, in admixture with a solid or liquid diluent or carrier, and may be administered orally, parenterally or rectally.</p> |
