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盐酸西替利嗪的合成工艺改进
引用本文:谭转云,向红琳,杨晓红,周海燕. 盐酸西替利嗪的合成工艺改进[J]. 中南药学, 2006, 4(5): 362-364
作者姓名:谭转云  向红琳  杨晓红  周海燕
作者单位:湖南师范大学医学院,长沙,410013
摘    要:目的改进盐酸西替利嗪的合成工艺。方法氯乙氧基乙酸乙酯制成碘乙氧基乙酸乙酯后与1-[(4-氯苯基)苯甲基]哌嗪缩合,再水解、成盐得到产品。结果所得产品达到药用标准,总收率60%。结论本合成中缩合反应条件被优化,收率提高,后处理简化,适合工业化生产。

关 键 词:盐酸西替利嗪  合成  碘乙氧基乙酸乙酯
文章编号:1672-2981(2006)05-0362-03
收稿时间:2006-01-04
修稿时间:2006-01-042006-04-19

Improvement on the synthesis of cetirizine dihydrochlorride
Tan Zhuan-yun,Xiang Hong-lin,Yang Xiao-hong,Zhou Hai-yan. Improvement on the synthesis of cetirizine dihydrochlorride[J]. Central South Pharmacy, 2006, 4(5): 362-364
Authors:Tan Zhuan-yun  Xiang Hong-lin  Yang Xiao-hong  Zhou Hai-yan
Affiliation:Medical College of Hunan Normal University, Changsha 410013
Abstract:OBJECTIVE To improve the synthesis of cetirizine dihydrochlorride.METHODS Cetirizine dihydrochlorride was prepared by the condensation reaction with ethyl 2-iodoethoxyacetate and 1-[(4-chlorophenyl)phenylmethyl]piperazine,and then followed by hydrolysis and salt formation with hydrochlororic acid.RESULTS The(overall) yield was 60%.CONCLUSIONS The condensation reaction was improved and could be used in mass production.
Keywords:cetirizine dihydrochlorride   synthesis   ethyl 2-iodoethoxyacetate
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