Cositecan, DB-172, BNP-1350, Karenitecin, -Drug Synthesis Database

【结构式】

【药物名称】Cositecan, DB-172, BNP-1350, Karenitecin

【化学名称】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

【CA登记号】203923-89-1

【分子式】C₂₅H₂₈N₂O₄Si

【分子量】448.59891

【开发单位】BioNumerik (Originator)

【药理作用】Brain Cancer Therapy, Lung Cancer Therapy, Melanoma Therapy, Non-Small Cell Lung Cancer Therapy, Oncolytic Drugs, Solid Tumors Therapy, Camptothecins, DNA Topoisomerase I Inhibitors, DNA-Intercalating Drugs

合成路线1

The title compound was prepared by radical addition of 3-(trimethylsilyl)propanal (II) to camptothecin (I) in the presence of FeSO4 and H2O2.

参考文献中间体

【1】 Haridas, K.; Hausheer, F.H.; Petluru, P.N.V.; Reddy, D.G.; Seetharamulu, P.; Murali, D.; Yao, S. (BioNumerik Pharmaceuticals, Inc.); Highly lipophilic camptothecin derivs.. WO 9835940 .

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	10816	Camptothecin; (4S)-4-Ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione; 4-et-4-hydroxy-1,12-dihydro-4h-2-oxa-6,12a-diaza-dibenzo(b,h)fluorene-3,13-dione	7689-03-4	C₂₀H₁₆N₂O₄	详情	详情
(II)	46476	3-(trimethylsilyl)propanal		C₆H₁₄OSi	详情	详情

Extended Information

Drug NewChemical Entity Original Patent(1)