CP-320626

Chemical Name: 5-Chloro-N-[1(S)-(4-fluorobenzyl)-2-(4-hydroxypiperidin-1-yl)-2-oxoethyl]-1H-indole-2-carboxamide
CAS No. 186430-23-9
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The reaction of N-(tert-butoxycarbonyl)-L-4-fluorophenylalanine (I) with 4-hydroxypiperidine (II) by means of triethylamine,EDC and HOBT in dichloromethane gives the expected piperidide (III),which is deprotected with with HCl in dioxane to afford (IV) with a free amino group that is condensed with 5-chloro-1H-indole-2-carboxylic acid (V) by means of triethylamine,EDC and HOBT as before.
📌 参考资料/链接:
参考文献标题:Substd.N-(indole-2-carbonyl)-glycinamides and derivs.as glycogen phosphorylase inhibitors
文献作者:Hulin,B.; Hoover,D.J.; Treadway,J.L.; Martin,W.H.; Phillips,D.(Pfizer Inc.)
参考来源:EP 0832065; WO 9639384

📄 详细内容


合成路线:The reaction of N-(tert-butoxycarbonyl)-L-4-fluorophenylalanine (I) with 4-hydroxypiperidine (II) by means of triethylamine,EDC and HOBT in dichloromethane gives the expected piperidide (III),which is deprotected with with HCl in dioxane to afford (IV) with a free amino group that is condensed with 5-chloro-1H-indole-2-carboxylic acid (V) by means of triethylamine,EDC and HOBT as before.
参考文献标题:Indole-2-carboxamide inhibitors of human liver glycogen phosphorylase
文献作者:Hoover,D.J.; Lefkowitz-Snow,S.; Burgess-Henry,J.L.; Martin,W.H.; Armento,S.J.; Stock,I.A.; McPherson,R.K.; Genereux,P.E.; Gibbs,E.M.; Treadway,J.L.
参考来源:J Med Chem 1998,41(16),2934


产品链接: CAS No. 186430-23-9››