【药物名称】BNP-1100
化学结构式(Chemical Structure):
参考文献No.40559
标题:Highly lipophilic camptothecin derivs.
作者:Seetharamulu, P.; Reddy, D.G.; Petluru, P.; Haridas, K.; Yao, S.; Hausheer, F.H.; Murali, D. (BioNumerik Pharmaceuticals, Inc.)
来源:WO 9807727
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.

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.

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