Dexloxiglumide, CR-2017
右氯谷胺Chemical Name: (R)-4-(3,4-Dichlorobenzamido)-5-[N-(3-methoxypropyl)-N-pentylamino]-5-oxopentanoic acid; N2-(3,4-Dichlorobenzoyl)-N1-(3-methoxypropyl)-N1-pentyl-D-aspartic acid 1-amide
CAS No. 119817-90-2
项目整合开发状态: Phase III
项目研究机构: Rotta (Originator), Forest (Licensee)
合成路线:The condensation of the N-(benzyloxycarbonyl)-D-glutamic acid 5-benzyl ester (I) with N-(3-methoxypropyl)-N-pentylamine (II) by means of ethyl chloroformate and triethylamine in THF gives the corresponding amide (III),which is debenzylated by hydrogenation over Pd/C in methanol,yielding compound (IV).Finally,the free amino group of (IV) is acylated with 3,4-dichlorobenzoyl chloride (V) by means of NaOH in water to give dexloxiglumide.
📌 参考资料/链接：
参考文献标题:Derivs.of (R)-5-pentylamino-5-oxopentanoic acid with anticholecystokinin activity
文献作者:Makovec,F.; Chiste,R.; Peris,W.; Rovati,L.(Rotta Research Laboratorium SpA)
参考来源:EP 0344184; JP 1988201156; US 5130474; US 5391574; WO 8805774
📄 详细内容
合成路线:The condensation of the N-(benzyloxycarbonyl)-D-glutamic acid 5-benzyl ester (I) with N-(3-methoxypropyl)-N-pentylamine (II) by means of ethyl chloroformate and triethylamine in THF gives the corresponding amide (III),which is debenzylated by hydrogenation over Pd/C in methanol,yielding compound (IV).Finally,the free amino group of (IV) is acylated with 3,4-dichlorobenzoyl chloride (V) by means of NaOH in water to give dexloxiglumide.
参考文献标题:Dexloxiglumide
文献作者:Castar,J.; Revel,L.; Makovec,F.
参考来源:Drugs Fut 1999,24(7),725
产品链接: CAS No. 119817-90-2››