2-[4-[(4-氯苯基)苯甲基]-1-哌嗪基]乙醇的合成

Synthesize research of 2-[4-[(4-chlorobenzyl)benzyl]-1-Piperazyl]ethanol

目的制备2-[4-[(4-氯苯基)苯甲基]-1-哌嗪基]乙醇。方法以氯苯和苯甲酰氯为起始原料,经付克反应、还原、氯化,再分别与哌嗪、氯乙醇、氯乙酸钠缩合,得到最终产物。结果合成目标产物的总收率为49.1%,中间体4-氯双苯酮,4-氯双苯甲醇,4-氯双苯氯甲烷,1-[(4-氯苯基)苯甲基]哌嗪为鲁南贝特制药有限公司生产确证。结论通过对合成路线的优化,使生产收率提高,降低成本,工艺更适于工业化的生产。

OBJECTIVE To synthesize 2 - [4- [ （4- chlorobenzyl） benzyl]- 1 - Piperazyl]ethanol. METHODS Cetiriz- ine hydrochloride was synthesized from chlorobenzene and benzoyl chloride by the Friedel-Crafts reaction, reduction, and chlo- rination followed by condensation with piperizine,chloroethanol on ehlorobenzene. RESULTS The yield of the target compound was improved to 49.1 %. All of the intermediates, such as 4-Chlorophenyl-phenyl methanone,4-Chlorobenzhydrol, 4-chloro- alpha- phenyl - benzenemethane, 1 - [ （ 4 - chlorophenyl） phenylmethyl] - piperazine were made in Lunan Pharmaceutical Better Limited Corporation. CONCLUSION The recycle rate was improved and the cost was decreased by changing the path of synthesis. And now the technique became suitful for the industrial production.