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【结 构 式】 
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【药物名称】Midostaurin, PKC-412, CGP-41251 【化学名称】N-[(9S,10R,11R,13R)-10-Methoxy-9-methyl-1-oxo-9,13-epoxy-2,3,10,11,12,13-hexahydro-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methylbenzamide 【CA登记号】120685-11-2 【 分 子 式 】C35H30N4O4 【 分 子 量 】570.65375 |
【开发单位】Novartis (Originator), Johns Hopkins University (Codevelopment) 【药理作用】Colorectal Cancer Therapy, ENDOCRINE DRUGS, Leukemia Therapy, Myeloid Leukemia Therapy, OCULAR MEDICATIONS, Oncolytic Drugs, Ophthalmic Drugs, Treatment of Age-Related Macular Degeneration, Treatment of Diabetic Complications, Angiogenesis Inhibitors, Flt3 (FLK2/STK1) Inhibitors, Inhibitors of Signal Transduction Pathways, Protein Kinase C (PKC) Inhibitors |
合成路线1
The title benzamide was prepared by acylation of the alkaloid staurosporine (I) with benzoyl chloride (II) in the presence of diisopropylethylamine in chloroform.
| 【1】 Caravatti, G.; et al.; Inhibitory activity and selectivity of staurosporine derivatives towards protein kinase C. Bioorg Med Chem Lett 1994, 4, 3, 399. |
| 【2】 Caravatti, G.; Fredenhagen, A. (Novartis AG); Staurosporine derivs. substd. for the nitrogen atom of the methylamino group. EP 0296110; JP 1989034989; US 5093330 . |