哌啶基氯代苯甲酰胺非肽类小分子的合成及表征

Synthesis and Characterization of Piperidinyl Chloro-Benzamide Non-Peptide Small Molecule

在介导HIV进入细胞受体的过程中,非肽类小分子具有重要的药理学意义,开发具有高活性、高选择性及良好药代动力学性质的新药已成为研究的热点,该类小分子具有氯原子、苯甲酰胺、哌啶等活性基团而备受关注.本文合成了哌啶苯甲酰胺的邻对位二取代、对位以及邻位氯化物(7);通过(7)、1-(对氯苯甲氧基)-2-溴甲基-4-溴苯(3)合成了三种新的哌啶基氯代苯甲酰胺类非肽类小分子8a-8c,对三种氯代苯甲酰胺进行了生物活性检测及IR、MS、1H NMR表征.结果表明N-乙基-4-氯-N-(N-(2-对氯苯甲氧基-5-溴苯甲基)-4-哌啶基)苯甲酰胺8a具有较好的生物活性.

Non- peptide small molecular has a great significance for pharmacology when mediated HIV goes into the cell receptor. It is necessary to develop novel drugs with high activity,high selectivity and good pharmacokinetic properties,which has become a hot spot. Among these small molecules,chlorine atomas group,benzamide and pyridine have attracted more research focus. In this paper,the intermediates（ 7）（ o,p- disubstituted,para and ortho benzamide piperidine chloride） are synthesized. Three benzamide chlorides are synthesized by the reaction of（ 7）with 2-（ bromomethyl）- 4- bromo- 1-（（ 4- chlorobenzyl） oxy） benzene（ 3）. These chloride are then characterized by biological activity and IR,MS,1H NMR. The results show that the N- ethyl- 4- chloro- N-（ 1-（ 5- bromo- 2-（（ 4- chlorophenmethyl） oxy） phenmethyl）- 4- piperidinyl） benzamide has a good biological activity.