论文部分内容阅读
为了研究结构和镇痛活性之间的关系,通过对吗啡类生物碱的结构改造,制备了大量的化合物。通常的改造方法之一,是将碱的N-甲基用其它烷基取代。吗啡(1,R~1=CH_3,R~2=H)和可待因(1,R~1=CH_3,R~2=CH_3)与溴化氰经Von Braun反应或氯甲酸烷基酯反应,可得到所需要的N-去甲吗啡(1,R~1=R~2=H)和N-去甲可待因(1,R~1=H,R~2=CH_3)。蒂巴因(2,R=CH_3)与偶氮二羧酸乙酯反应后经水解,可得到N-去甲蒂巴因(2,R=H)。
In order to study the relationship between structure and analgesic activity, a large number of compounds were prepared by structural modification of morphine alkaloids. One of the common reworking methods is to substitute the N-methyl group of the base with other alkyl groups. Morphine (1, R 1 = CH 3, R 2 = H) and codeine (1, R 1 = CH 3, R 2 = CH 3) are reacted with cyanogen bromide via Von Braun reaction or alkyl chloroformate The desired N-desmethyl morphine (1, R ~ 1 = R ~ 2 = H) and N-desmethylcodeine (1, R ~ 1 = H, R ~ 2 = CH_3) were obtained. The reaction of Tibaine (2, R = CH_3) with ethyl azodicarboxylate followed by hydrolysis gives N-destibaine (2, R = H).