【摘要】 本文报导了不同N-苯乙基甘氨酸衍生物在Lewis酸催化下的分子内环化反应的若干规律,以及苯并-3-氮杂环庚酮-1衍生物的合成.更多还原

【Abstract】 The intramolecular cyclization of some iV-piperonylglycine derivatives under the catalysis of Lewis acids was studied. In example 3a, in which the nitrogen atom was not protected, under the action of（CF₃CO）₂O-CF₃COOH, 3a was converted into 3c, 3-ethyl-8, 9-methylenedioxy-10b-trifluoromethyl-2, 3, 5, 6-tetrahydro-10bHoxazolo（2, 3-a）-isoquinoline, instead of 3b. The structure of 3c was identified through IR, ¹³CNMR and also through the identification of its hydrolytic product 3d and the methyl ester 3e.However, if the nitrogen atom was protected as in the case of 4a and 5a, the major products N-p-toluenesulphonyl-7,8-methylenedioxy-1, 2,4, 5-tetrahydrobenzazepin-3-one-1 （4 b） and N-p-methoxyphenylsulphony1-7, 8-methylenedioxy-1,2, 4, 5-tetrahydrobenzazepin-3-one-1（5b） were obtained respectively, and at the same time, a minor product, N-p-toluenesulphonyl-6, 7-methylenedioxy-1, 2, 3, 4-tetrahydroisoquinoline（4c） and N-p-methoxyphenylsulphonyl-6, 7-methylenedioxy-1, 2, 3, 4-tetrahydroisoquinoline （5c） were isolated. For lack of an activating group on benzene ring in 6a, only the formation of N-p-toluenesulphonylisoquinoline（6c） was obtained （structural formulae see Chinese text）.更多还原