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【结 构 式】 
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【药物名称】 【化学名称】(6R,8S,9R)-N-[4-Amino-9-(tert-butyldimethylsilyloxy)-6-(tert-butyldimethylsilyloxymethyl)-1,7-dioxa-2-thiaspiro[4.4]-3-nonen-8-y]-N'-phenylurea S,S-dioxide 【CA登记号】 【 分 子 式 】C26H45N3O7SSi2 【 分 子 量 】599.90045 |
【开发单位】CSIC (Originator), Rega Institute for Medical Research (Originator) 【药理作用】AIDS Medicines, Anti-HIV Agents, ANTIINFECTIVE THERAPY, Reverse Transcriptase Inhibitors |
合成路线1
The reduction of azide (I) with trimethylphosphine in THF gives the amine (II), which is then treated with phenyl isocyanate (A) in acetonitrile yielding a mixture of alpha and beta phenylureas which is separated by centrifugal circular thin layer chromatography.
| 【1】 Velázquez, S.; Chamorro, C.; Perez-Perez, M.J.; Alvarez, R.; Jimeno, M.L.; Martin-Domenech, A.; Perez, C.; Gago, F.; De Clercq, E.; Balzarini, J.; San-Felix, A.; Camarasa, M.J.; Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase. J Med Chem 1998, 41, 23, 4636. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (A) | 11289 | 1-Isocyanatobenzene; phenyl isocyanate; Phenylisocyanate | 103-71-9 | C7H5NO | 详情 | 详情 |
| (I) | 26923 | (6R,8R,9R)-4-amino-8-azido-9-[[tert-butyl(dimethyl)silyl]oxy]-6-([[tert-butyl(dimethyl)silyl]oxy]methyl)-1,7-dioxa-2lambda(6)-thiaspiro[4.4]non-3-ene-2,2-dione | C19H38N4O6SSi2 | 详情 | 详情 | |
| (II) | 26924 | (6R,8R,9R)-4,8-diamino-9-[[tert-butyl(dimethyl)silyl]oxy]-6-([[tert-butyl(dimethyl)silyl]oxy]methyl)-1,7-dioxa-2lambda(6)-thiaspiro[4.4]non-3-ene-2,2-dione | C19H40N2O6SSi2 | 详情 | 详情 |
Extended Information