促动力药西沙必利合成工艺的改进
Improved synthesis of prokinetics Cisapride
作者：张善军;蒋琳;
Author：
收稿日期： 年卷（期）页码：2010,25(04):-392-393
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：促动力药;西沙必利;合成工艺改进
Key words：
基金项目：
中文摘要
目的改进促动力药西沙必利的合成工艺。方法以N-Boc-4-哌啶酮为原料,经羟基化、甲基化、脱保护、缩合、还原氨化等9步反应合成促动力药西沙必利。结果与结论通过工艺改进,使总收率由4.5%提高到17%,产物结构经1HNMR、MS分析确证。
参考文献
[1]McKinnell RM,Armstrong SR,Beattie DT,et al.A multivalent approach to the design and discovery of orally efficacious5-HT4receptor agonists[J].J Med Chem,2009,52(17):5330-5343.
[2]Cossy J,Molina JL,Desmurs JR.A short synthesis of cisapride:a gastrointestinal stimulant derived from cis-4-amino-3-methoxypiperdine[J].Tetrahedron Lett,2001,42(33):5713-5715.
[3]Lee JS,Oh YS,Yang WY,et al.Benzotriazol-1-yl alkyl car-bonate,a new convenient and inexpensive coupling agent for preparation of an active ester in the synthesis of an amide[J].Synthetic Communications,1999,29(14):2547-2557.
[4]Janssen CGM,Lenoir HAC,Thijssen JJA,et al.Synthesis of3H and14C-Cisapride[J].J Labelled Compounds and Radiophar-maceuticals,1987,24(12):1493-1501.
[5]V Daele,Georges HP,D Bruyn,et al.Synthesis of cisapride,a gastrointestinal stimulant derived from cis-4-amino-3-me-thoxypiperidine[J].Drug Develop Res,1986,8(1):225-232.
【关闭】
