|
【结 构 式】 
|
【药物名称】 【化学名称】[1R,9S,12S(1'R,3'R,4'R),13R,14S,17R,21S,23S,24R,25S,27R]-17-Ethyl-1,14-dihydroxy-23,25-dimethoxy-12-[2(E)-[3-methoxy-4-(3-phenylcarbazoyloxy)cyclohexyl]-1-methylvinyl]-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0(4,9)]octacos-18(E)-ene-2,3,10,16-tetraone 【CA登记号】220873-56-3 【 分 子 式 】C50H75N3O13 【 分 子 量 】926.16755 |
【开发单位】Novartis (Originator) 【药理作用】Antiallergy/Antiasthmatic Drugs, Asthma Therapy, IMMUNOMODULATING AGENTS, Immunosuppressants, RESPIRATORY DRUGS |
合成路线1
The title compound was obtained by treatment of ascomycin (I) with triphosgene and 4-dimethylaminopyridine at -78 C to produce selectively the 32-hydroxyl mono-acylated product (II), which was subsequently condensed with phenylhydrazine yielding the target phenylcarbazate.
| 【1】 Hersperger, R.; et al.; Preparation and immunosuppressive activity of 32-(O)-acylated and 32-(O)-thioacylated analogues of ascomycin. Bioorg Med Chem Lett 1999, 9, 2, 227. |
| 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) | 14951 | (1R,9S,12S,13R,14S,17R,21S,23S,24R,25S,27R)-17-ethyl-1,14-dihydroxy-12-[(E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0(4,9)]octacos-18-ene-2,3,10,16-tetron | C43H69NO12 | 详情 | 详情 | |
| (II) | 30247 | (1R,9S,12S,13R,14S,17R,21S,23S,24R,25S,27R)-12-((E)-2-[(1R,3R,4R)-4-[(chlorocarbonyl)oxy]-3-methoxycyclohexyl]-1-methylethenyl)-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-2,3,10,16-tetraoxo-11,28-dioxa-4-azatricyclo[22.3.1.0(4,9)]octacos-18-ene | C44H68ClNO13 | 详情 | 详情 |