BNP-1100
Chemical Name: 4(S)-Ethyl-4-hydroxy-11-(methylsulfanyl)-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione; 7-(Methylsulfanyl)camptothecin
CAS No. 203923-75-5
项目整合开发状态: Biological Testing
项目研究机构: BioNumerik (Originator)
合成路线: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.
📌 参考资料/链接：
参考文献标题:Highly lipophilic camptothecin derivs.
文献作者:Seetharamulu,P.; Reddy,D.G.; Petluru,P.; Haridas,K.; Yao,S.; Hausheer,F.H.; Murali,D.(BioNumerik Pharmaceuticals,Inc.)
参考来源:WO 9807727
📄 详细内容
合成路线: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: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.
参考文献标题:Highly lipophilic camptothecin derivs.
文献作者:Haridas,K.; Hausheer,F.H.; Petluru,P.N.V.; Reddy,D.G.; Seetharamulu,P.; Murali,D.; Yao,S.(BioNumerik Pharmaceuticals,Inc.)
参考来源:WO 9835940