| 摘要 |
<p>The invention comprises 3-hydroxy-5-aminomethylisoxazole and its acid addition salts, pharmaceutical preparations containing them, and their preparation by (a) reducing a compound of the formula <FORM:1034939/C2/1> (wherein R represents a hydrogen atom or benzyl group), (b) hydrogenolysing 3-benzyloxy-5-aminomethylisoxazole, (c) heating a compound of the formula <FORM:1034939/C2/2> (wherein R11 represents an alkyl group containing not more than four carbon atoms or a benzyl group) with hydrobromic or hydrochloric acid, pyridine hydrobromide or hydrochloride or an alkylpyridine hydrobromide or hydrochloride, (d) reacting a reactive ester of 3 - hydroxy - 5 - hydroxymethylisoxazole with ammonia, or (e) hydrolysing a compound of the formula <FORM:1034939/C2/3> (wherein Ac represents an acyl group containing not more than seven carbon atoms), optionally followed in each case by acid addition salt formation. The preparation of 3-methoxy-5-bromomethyl-isoxazole, 3 - methoxy - 5 - azidomethylisoxazole, 3 - hydroxy - 5 - azidomethylisoxazole, methyl g - chloro - b ,b - dimethoxybutyrate, g - chloro-b ,b -dimethoxybutyrohydroxamic acid, 3-hydroxy-5 - chloromethylisoxazole, 3 - benzyloxy - 5-acetamidomethylisoxazol and 3 - hydroxy - 5-acetamidomethylisoxazole is described. The compounds of the invention strongly potentiate anaesthetics, reduce motility, have catatonic and sedative effects, inhibit the tremorine tremor and have an anti-emetic action. They may be administered in the form of pharmaceutical preparations containing them together with a carrier.</p> |
