|
【结 构 式】 
|
【药物名称】KNI-685 【化学名称】3'-Azido-5'-O-[3-[N-[1(S)-benzyl-2(S)-[4(R)-(N-tert-butylcarbamoyl)-5,5-dimethylthiazolidin-3-ylcarbonyl]-2-hydroxyethyl]carbamoyl]-2-methylbutyryl]-3'-deoxythymidine 【CA登记号】 【 分 子 式 】C36H50N8O9S 【 分 子 量 】770.9121 |
【开发单位】Kyoto Pharmaceutical University (Originator) 【药理作用】AIDS Medicines, Anti-HIV Agents, ANTIINFECTIVE THERAPY, HIV Protease Inhibitors, Reverse Transcriptase Inhibitors |
合成路线1
The condensation of azidothymidine (I) with 2,3-dimethylsuccinic anhydride (II) afforded amide (III). This was then coupled with amine (IV) using DCC and HOBt to furnish the title compound.
| 【1】 Kiso, Y.; Kimura, T.; Akaji, K.; Matsuda, T.; Matsumoto, H.; Hamawaki, T.; A new class of potent anti-HIV agents, conjugates of HIV protease inhibitors containing carboxylic acid with reverse transcriptase inhibitor. Symp Med Chem 1998, Abst 1-P-17. |
| 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) | 25317 | 1-[(2R,4S,5S)-4-azido-5-(hydroxymethyl)tetrahydro-2-furanyl]-5-methyl-2,4(1H,3H)-pyrimidinedione | 101703-35-9 | C10H13N5O4 | 详情 | 详情 |
| (II) | 29297 | 3,4-dimethyldihydro-2,5-furandione | C6H8O3 | 详情 | 详情 | |
| (III) | 29298 | 4-([(2S,3S,5R)-3-azido-5-[5-methyl-2,4-dioxo-3,4-dihydro-1(2H)-pyrimidinyl]tetrahydro-2-furanyl]methoxy)-2,3-dimethyl-4-oxobutyric acid | C16H21N5O7 | 详情 | 详情 | |
| (IV) | 29294 | (4R)-3-[(2S,3S)-3-amino-2-hydroxy-4-phenylbutanoyl]-N-(tert-butyl)-5,5-dimethyl-1,3-thiazolidine-4-carboxamide | C20H31N3O3S | 详情 | 详情 |
Extended Information