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刘维勤等曾研究β位取代桂皮酰胺类化合物的抗惊厥活性.为了深入研究β位取代基位阻效应对桂皮酰胺类化合物抗惊厥活性的影响,我们合成了-系列N-(β-氨基-4-氯桂皮酰基)仲丁胺类化合物. 在氢化钠存在下,对氯苯乙酮与碳酸二乙酯缩合,生成对氯苯甲酰基乙酸乙酯.后者经水解、酸化得相应的羧酸.羧酸在室温下用草酰氯进行酰氯化,然后用仲丁胺氨解,得到N-(β-羟基-4-氯桂皮酰基)仲丁胺(3)
Liu Weiqin et al studied the anticonvulsant activity of β-substituted cinnamides.In order to study the effect of steric hindrance of β-substituent on the anticonvulsant activity of cinnamides, we synthesized a series of N- (β-amino-4 - chloro cinnamoyl) sec-butylamine compounds in the presence of sodium hydride, p-chloroacetophenone and diethyl carbonate condensation, resulting in p-chlorobenzoyl ethyl acetate, the latter by hydrolysis, acidification to the corresponding carboxylic acid . The carboxylic acid is chlorinated with oxalyl chloride at room temperature and then aminocamidated to give N- (β-hydroxy-4-chlorocinnamyl) sec-butylamine (3)