新产品编号:1614149
Chemical Name: (5R,5aR,8aS,9S)-9-[4-(1H-Benzimidazol-2-yl)phenylamino]-5-(4-hydroxy-3,5-dimethoxyphenyl)-5,8,8a,9-tetrahydrofuro[3',4':6,7]naphtho[2,3-d][1,3]dioxol-6(5aH)-one
项目整合开发状态: Preclinical
项目研究机构: Genelabs (Originator)
合成路线:Oxidative oxidation of p-nitrobenzaldehyde (I) and 1,2-phenylenediamine (II) in DMF in the presence of nitrobenzene produced benzimidazole (III).Subsequent reduction of the nitro group of (III) by means of NaBH4 and CuCl afforded aniline (IV).Bromide (VI) was prepared by treatment of 4'-demethyl epipodophyllotoxin (V) with HBr.The title compound was then obtained by coupling aniline (IV) with bromide (VI) using BaCO3 in 1,2-dichloroethane.
📌 参考资料/链接:
参考文献标题:Antitumor agents.194.Synthesis and biological evaluations of 4-beta-mono-,-di-,and -trisubstituted aniline-4'-O-demethyl-podophyllotoxin and related compounds with improved pharmacological profiles
文献作者:Zhu,X.K.; Guan,J.; Tachibana,Y.; Bastow,K.F.; Cho,S.J.; Cheng,H.H.; Cheng,Y.C.; Gurwith,M.; Lee,K.H.
参考来源:J Med Chem 1999,42(13),2441