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【结 构 式】 
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【药物名称】KT-6352 【化学名称】9,13-Epoxy-10-methoxy-2,9-dimethyl-11-(methylamino)-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-1-one 【CA登记号】161510-80-1 【 分 子 式 】C29H28N4O3 【 分 子 量 】480.57151 |
【开发单位】Kyowa Hakko (Originator) 【药理作用】Antithrombocytopenic, Chemoprotective Agents, HEMATOLOGIC DRUGS, Hematopoiesis Disorders Therapy, ONCOLYTIC DRUGS, Radioprotectants |
合成路线1
The known antibiotic staurosporine (I) was protected as the N-benzyloxycarbonyl derivative (II) by treatment with benzyl chloroformate in the presence of NaHCO3. Subsequent alkylation of (II) at the 2-N atom by treatment with iodomethane and NaH in DMF provided the N-methyl derivative (III). Finally, deprotection of the benzyloxycarbonyl group of (III) by hydrogenation over Pd/C furnished the title compound.
| 【1】 Murakata, C.; Sato, A.; Kasai, M.; Morimoto, M.; Akinaga, S. (Kyowa Hakko Kogyo Co., Ltd.); Staurosporin derivatives. EP 0383919; JP 2766360B2; WO 8907105 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 10101 | Benzyloxycarbonyl chloride; Benzyl chloroformate; 1-[[(Chlorocarbonyl)oxy]methyl]benzene | 501-53-1 | C8H7ClO2 | 详情 | 详情 | |
| (I) | 36327 | 3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1(2,6).0(7,28).0(8,13).0(15,19).0(20,27).0(21,26)]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | 62996-74-1 | C28H26N4O3 | 详情 | 详情 |
| (II) | 36328 | benzyl 3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1(2,6).0(7,28).0(8,13).0(15,19).0(20,27).0(21,26)]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl(methyl)carbamate | C36H32N4O5 | 详情 | 详情 | |
| (III) | 36329 | benzyl 3-methoxy-2,17-dimethyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1(2,6).0(7,28).0(8,13).0(15,19).0(20,27).0(21,26)]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl(methyl)carbamate | C37H34N4O5 | 详情 | 详情 |