DB-172, BNP-1350, Karenitecin-药物合成数据库

【药物名称】DB-172, BNP-1350, Karenitecin

化学结构式(Chemical Structure):

参考文献No.	40560
标题:	Highly lipophilic camptothecin derivs.
作者:	Haridas, K.; Hausheer, F.H.; Petluru, P.N.V.; Reddy, D.G.; Seetharamulu, P.; Murali, D.; Yao, S. (BioNumerik Pharmaceuticals, Inc.)
来源:	WO 9835940

合成路线图解说明: The title compound was prepared by radical addition of 3-(trimethylsilyl)propanal (II) to camptothecin (I) in the presence of FeSO4 and H2O2.

合成路线图解说明: Reaction of 20-O-acetylcamptothecinone (I) with trifluoromethanesulfonic anhydride and pyridine afforded triflate (II). Subsequent displacement of the triflate group of (II) by methanethiol in the presence of diisopropylethylamine gave 20-O-acetyl-7-(methylthio)camptothecin (III). Finally, the acetate ester was hydrolyzed by treatment with K2CO3 in MeOH to yield the title compound.