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寻找研究无镇静作用的H_1受体拮抗药在制药工业已获成效,已有几个无镇静作用的H_1受体抗组胺药用于临床,其余尚在研究中,其中包括cetirizine,为一羟嗪的人体代谢物。是一个作用强而持久,且具选择性的抗H_1受体特性,而无镇静副作用的新的抗过敏药。合成 1-(4-氯二苯甲基)哌嗪(Ⅰ)与2-(2-氯乙氧基)醋酸甲酯(Ⅱ)经加碳酸钠在二甲苯中回流缩合,生成2-〔2-〔4-(4-氯二苯甲基)-1-哌嗪基〕乙氧基〕醋酸甲酯(Ⅲ),然后Ⅲ在乙醇内回流,经氢氧化钾水解而得
Looking to study the no-sedating H 1 receptor antagonist has been effective in the pharmaceutical industry. Several sedative H 1 -receptor antihistamines have been used clinically, with the remainder being studied, including cetirizine, Triazine metabolites. Is a potent, long-lasting, and new antiallergic agent with selective anti-H-1 receptor properties without sedating side effects. Synthesis of methyl 1- (4-chlorobenzhydryl) piperazine (I) and methyl 2- (2-chloroethoxy) acetate were reflux condensation in the presence of sodium carbonate to give 2- [2 - [4- (4-chlorobenzhydryl) -1-piperazinyl] ethoxy] acetate (III) followed by refluxing in ethanol to give