DB-172, BNP-1350, Karenitecin

(4S)-4-乙基-4-羟基-11-(2-三甲基硅基)乙基)-1H-吡喃并[3',4':6,7]氮茚并[1,2-B]喹啉-3,14(4H,12H)-二酮Chemical Name: 7-[2-(Trimethylsilyl)ethyl]-20(S)-camptothecin; 4(S)-Ethyl-4-hydroxy-11-[2-(trimethylsilyl)ethyl]-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
CAS No. 203923-89-1
项目整合开发状态: Phase II
项目研究机构: BioNumerik (Originator)
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.