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【结 构 式】 
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【药物名称】Daptomycin, LY-146032, Cubicin, Cidecin, Dapcin 【化学名称】N-(1-Oxodecyl)-L-tryptophyl-L-asparaginyl-L-aspartyl-L-threonyl-glycyl-L-ornithyl-L-aspartyl-D-alanyl-L-aspartyl-glycyl-D-seryl-threo-3-methyl-L-glutamyl-gamma-(2-aminophenyl)-gamma-oxo-L-alpha-aminobutyric acid C-1.13-O-2.4-lactone 【CA登记号】103060-53-3 【 分 子 式 】C72H101N17O26 【 分 子 量 】1620.70607 |
【开发单位】Lilly (Originator), Chiron (Licensee), Cubist (Licensee), Emisphere (Formulation) 【药理作用】Antibiotics, ANTIINFECTIVE THERAPY |
合成路线1
A-21978C nucleus (I) (obtained by deacylating A-21978C complex by fermentation with Actinoplanes utahensis NRRL 12052) is protected with di-tert-butyl carbonate (II) and NaOH in water to give the N-(Orn-)-tert-butoxycarbonyl derivative (III), which is treated with 2,4,5-trichlorophenyl decanoate (IV) in hot DMF yielding the protected decanoyl derivative (V). Finally, this compound is deprotected with trifluoroacetic acid / 1,2-ethanedithiol.
| 【1】 Abbott, B.J.; Debono, M.; Fukuda, D.S. (Eli Lilly and Company); Derivs. of A-21978C cyclic peptides. US 4537717 . |
| 【2】 Dionisi, M.S.; Patoia, L.; Castaner, J.; Daptomycin. Drugs Fut 1991, 16, 7, 608. |