安徽医药
安徽醫藥
안휘의약
ANHUI MEDICAL AND PHARMACEUTICAL JOURNAL
2014年
6期
1028-1029,1030
,共3页
萘哌地尔%TEBA%合成
萘哌地爾%TEBA%閤成
내고지이%TEBA%합성
naftopidil%TEBA%synthesis
目的:研究萘哌地尔的合成工艺。方法以1-萘酚和环氧氯丙烷为原料,在相转移催化剂TEBA作用下反应,再与间甲氧基苯基哌嗪作用,生成萘哌地尔。结果萘哌地尔的最佳合成条件为:化合物Ⅰ与化合物Ⅱ的摩尔比为1∶1,反应温度为60℃。结论该方法有合成路线简单、反应条件温和、产物易精制等优点,完全适合工业化生产。
目的:研究萘哌地爾的閤成工藝。方法以1-萘酚和環氧氯丙烷為原料,在相轉移催化劑TEBA作用下反應,再與間甲氧基苯基哌嗪作用,生成萘哌地爾。結果萘哌地爾的最佳閤成條件為:化閤物Ⅰ與化閤物Ⅱ的摩爾比為1∶1,反應溫度為60℃。結論該方法有閤成路線簡單、反應條件溫和、產物易精製等優點,完全適閤工業化生產。
목적:연구내고지이적합성공예。방법이1-내분화배양록병완위원료,재상전이최화제TEBA작용하반응,재여간갑양기분기고진작용,생성내고지이。결과내고지이적최가합성조건위:화합물Ⅰ여화합물Ⅱ적마이비위1∶1,반응온도위60℃。결론해방법유합성로선간단、반응조건온화、산물역정제등우점,완전괄합공업화생산。
Objective To study the synthesis process of naftopidil.Methods Naftopidil was successfully synthesized using 1-naphthol and epichlorohydrin as materials.The two materials firstly reacted in the presence of phase transfer catalyst TEBA,then directly reac-ted with 1-(3-methoxyphenyl)piperazine.Results The optimal synthesis conditions of naftopidil:molar ratio of productⅠandⅡis 1∶1 ,reaction temperature is 60℃.Conclusions The synthetic route of the process is simple,the reaction conditions were mild,the product is easily purified,and the process is very suitable for industrialization.