非肽类小分子拮抗剂苯甲酰胺衍生物的合成及表征

Synthesis and haracterization of non-peptide small molecular antagonist benzamide derivatives

本实验以4-氯苄氯、5-溴水杨醛为原料,通过消去、还原及溴化合成了5-溴-2-(4-氯苄氧基)溴甲基苯(Ⅲ),以1-苄基-4-哌啶酮合成了N-丙基-N-(4-哌啶基)苯甲酰胺(Ⅳ),通过Ⅲ、Ⅳ合成了一种新的非肽类小分子化合物CCR5拮抗剂苯甲酰胺衍生物,对该拮抗剂进行了1H NMR、13C NMR及MS表征,同时,对产物进行了生物活性测试.

5-bromo-2-（（4-chlorobenzyl）oxy）bromomethyl benzene （III）was synthesized from 1-chloro-4-（chloromethyl）benzene and 5-bromo-2-hydroxybenzaldehyde by eliminationreaction,reduction reaction and bromization.N-（piperidine-4-yl）-N-propylbenzamide （IV）was prepared from 1-benzylpip-eridine-4-one.Further reaction of III with IV gave a novelnon-peptide CCR5 antagonist Benzamide deriva-tives.The structure of these products was characterized by 1HNMR,13CNMR and MS,and The products were tested for biological activity.