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【结 构 式】 
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【药物名称】 【化学名称】N-Decanoyl-L-tryptophyl-L-asparaginyl-L-aspartyl-Lthreonyl- glycyl-N5-(1H-imidazol-2-ylmethyl)-L-ornithyl-Laspartyl- D-alanyl-L-aspartyl-glycyl-D-seryl-threo-3-methyl- L-glutamyl-3-anthraniloyl-L-alanine C-1.13-O-2.4-lactone 【CA登记号】345645-14-9 【 分 子 式 】C76H105N19O26 【 分 子 量 】1700.79595 |
【开发单位】Cubist (Originator) 【药理作用】Antibiotics, ANTIINFECTIVE THERAPY |
合成路线1
The title compound is prepared by reductive alkylation of daptomycin (I) with 2 imidazolecarboxaldehyde (II) in the presence of NaBH(OAc)3 in DMF.
| 【1】 Yu, X.Y.; et al.; Synthesis and biological activity of ornithine heterocyclic analogs of daptomycin. 42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002, San Diego) 2002, Abst F-349. |
| 【2】 Watson, A.D.; Hill, J.; Zhang, Y.; Finn, J.; Yu, X.Y.; Keith, D.; Morytko, M.; Parr, I.; Siedlecki, J.; Silverman, J.; Christensen, D.; Lazarova, T. (Cubist Pharmaceuticals, Inc.); Lipopeptides as antibacterial agents. WO 0144274 . |
| 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) | 61989 | (3S)-3-[((2S)-4-amino-2-{[(2S)-2-(decanoylamino)-3-(1H-indol-3-yl)propanoyl]amino}-4-oxobutanoyl)amino]-4-({(3S,6S,9R,15S,18R,21S,24S,30S,31R)-3-[2-(2-aminophenyl)-2-oxoethyl]-24-(3-aminopropyl)-15,21-bis(carboxymethyl)-9-(hydroxymethyl)-6-[(1R)-3-h | C72H101N17O26 | 详情 | 详情 | |
| (II) | 41148 | 1H-imidazole-2-carbaldehyde | 10111-08-7 | C4H4N2O | 详情 | 详情 |
Extended Information