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1.环己酮与草酸二乙酯起缩合作用,生成物加热失去一氧化碳,生成2-乙氧羰基-环己酮。此酮与叠氮化钠起 Schmidt 反应,生成2-乙氧羰基-7-酮-氮七圜。此氮七圜用氢化铝锂还原,成2-羟甲基氮七圜。此化合物与三氯甲醛起反应,生成物再用氢化铝锂还原,成1-甲基-2-羟甲基氮七圜。2.1-甲基-2-羟甲基氮七圜的衍生物,皆用通常方法制备,其对氨基苯甲酸酯盐酸盐因刺激性强,未宜作局部麻醉药用。其他化合物药理试验结果未详。3.利用环庚酮为原料,用上述的反应程序,制备1-甲基-2-羟甲基氮八圜。此化合物的衍生物皆可用通常方法制备。其对氮基苯甲酸酯盐酸盐及其二苯基乙酸酯的溴甲烷季铵盐的药理试验结果亦未详。
1. Cyclohexanone and diethyl oxalate from condensation, the resultant heated to lose carbon monoxide, generating 2-ethoxycarbonyl - cyclohexanone. This ketone and sodium azide Schmidt reaction to generate 2-ethoxycarbonyl-7-one - nitrogen seven 圜. This nitrogen seven 圜 lithium aluminum hydride reduction, into 2 - hydroxymethyl nitrogen seven 圜. This compound reacts with trichlorofluric acid and the product is reduced with lithium aluminum hydride to give 1-methyl-2-hydroxymethyl-7-azabicyclo. 2.1-methyl-2-hydroxymethyl nitrogen seven 圜 derivatives, are prepared by the usual method, the para-aminobenzoate hydrochloride due to irritation, not suitable for local anesthetic use. Other compounds pharmacological test results are not available. 3. Using cycloheptanone as starting material, using the above reaction procedure, 1-methyl-2-hydroxymethyl nitrogen eight 圜. Derivatives of this compound can be prepared by conventional methods. Its p-nitrobenzoate hydrochloride and diphenyl acetate methyl bromide quaternary ammonium pharmacological test results are not yet available.