Dong Chuan-min
2014
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Journal
Coal and Chemical Industry
Abstract
1-[(4-chlorophenyl)phenyl methyl] piperazine,the key intermediate of cetirizine hydrochloride,was synthesized from 4-chlorobenzophenone via reduction with zinc dust,bromination with hydrogen bromide and final reaction with anhydrous piperazine.The optimum reaction conditions were obtained as follow:molar ratio of reagent(zinc/4-chlorobenzophenone) was 2.5;bromination temperature was between 75~80 ℃,and temperature of piperazine reaction was between 80~85 ℃.The final product(HPLC 98.7%) was prepared with an overall yield of 71.2%.The materials of this route were cheap and common and it was suitable for industrial production.