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P.A.J.Janssen 等于六十年代初合成了一系列4-苯胺基哌啶类衍生物,其中以芬太尼(fentanyl)最为著称,它的镇痛强度约为吗啡200倍左右。为了进一步探索4-苯胺基哌啶类衍生物的化学结构与镇痛作用之间的关系,作者合成了一系列芬太尼类衍生物,其化学结构改造分下列四类(见下图)。在本工作中,还研究了用氯甲酸甲酯使 N-苄基转变为氨基甲酸酯,然后用5%NaOH 水溶液水解脱羧的新的脱苄方法,产量较好。
P.A.J.Janssen equal to the early sixties synthesized a series of 4-anilino piperidine derivatives, of which fentanyl is most known, its analgesic strength is about 200 times that of morphine. In order to further explore the relationship between the chemical structure and the analgesic effect of 4-anilinopiperidine derivatives, the authors synthesized a series of fentanyl derivatives, the chemical structure of the following four categories (see below). In this work, a new debenzylation method using methyl chloroformate to convert N-benzyl to carbamate followed by hydrolytic decarboxylation with 5% aqueous NaOH was also studied, yielding better.