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用三种麻黄碱和芳醛反应合成28个2-芳基-3,4-二甲基-5-苯基噁唑烷类和Schiff碱类化合物。根据前药原理用UV和HPLC法探讨了立体结构和水解动力学的问题,测得生理条件下的水解半寿期,初步阐明了空间效应对稳定性的影响以及Hammett取代基常数与水解速率的规律。实验表明此类噁唑烷衍生物作为麻黄碱的前药有理论和应用价值。
Two 2-aryl-3,4-dimethyl-5-phenyloxazolidines and Schiff base compounds were synthesized by reaction of three kinds of ephedrine with aromatic aldehydes. According to the principles of prodrugs, the problems of the three-dimensional structure and hydrolysis kinetics were investigated by UV and HPLC. The half life of hydrolysis under physiological conditions was measured. The effects of steric effect on stability and Hammett substituent constants and hydrolysis rates law. Experiments show that these oxazolidine derivatives as ephedrine prodrugs have theoretical and practical value.