PS-1145
N-(6-氯-9H-beta-咔啉-8-基)烟酰胺Chemical Name: N-(6-Chloro-9H-pyrido[3,4-b]indol-8-yl)pyridine-3-carboxamide; N-(6-Chloro-9H-beta-carbolin-8-yl)pyridine-3-carboxamide
CAS No. 431898-65-6, 431898-66-7 (monotrifluoroacetate)
项目整合开发状态: Preclinical
项目研究机构: Aventis Pharma (Originator), Millennium (Not Determined)
合成路线:The chlorination of norharmane (I) by means of N-chlorosuccinimide in aqueous HCl affords 7-chloro-beta-carboline (II).Subsequent electrophilic nitration of (II) with concentrated HNO3 gives rise to the 9-nitro compound (III),which is further reduced to the corresponding amine (IV) with SnCl2/HCl.Acylation of amine (IV) with nicotinoyl chloride (V) in pyridine then furnishes the target nicotinamide derivative.
📌 参考资料/链接:
参考文献标题:Substd.beta-carbolines as IkB-kinase inhibiting activity
文献作者:Adams,J.; Soucy,F.; Grenier,L.; Castro,A.; Mazdiyasni,H.; Hancock,W.W.; Ritzeler,O.; Palombella,V.(Aventis Pharma Deutschland GmbH)
参考来源:EP 1134221; EP 1209158; EP 1268477; JP 2003527394; US 2002099068; US 6627637; WO 0168648