为了研究具有选择性的多巴胺(DA)受体拮抗剂,合成了一系列N-(1-乙基-2-哌咯烷基甲基)苯甲酰胺类新化合物。其中若干化合物具有比舒必利更强的阻滞DA受体的作用,呈现活性的化合物大多是S-构象的左旋体,如本文介绍的remoxipride。合成 2,6-二甲氧基苯甲酸经溴化后生成3-溴-2,6-二甲氧基苯甲酸,再与二氯亚砜回流,得到相应的酰氯化物,最后与(一)- In order to study the selective dopamine (DA) receptor antagonists, a series of novel N- (1-ethyl-2-piperidinylmethyl) benzamide compounds were synthesized. Several of these compounds have a more potent DA receptor blocking effect than sulpiride, and most of the compounds that exhibit activity are S-conformation levans, such as the remoxipride described herein. The synthesis of 2,6-dimethoxybenzoic acid by bromination to generate 3-bromo-2,6-dimethoxybenzoic acid, and then refluxed with thionyl chloride to give the corresponding acid chloride, and finally with (a) -