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【结 构 式】 
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【药物名称】 【化学名称】N-[3(R)-Hydroxytetradecanoyl]-L-seryl-N4-(isopropylcarbonyloxymethoxycarbonyl)-D-(2,4-diaminobutyryl)-N4-(cyclopropyl)-L-asparaginyl-N4-(isopropylcarbonyloxymethoxycarbonyl)-L-lysyl-N4-(isopropylcarbonyloxymethoxycarbonyl)-L-(2,4-diaminobutyryl)-L-allothreonyl-(Z)-2,3-didehydro-2-aminobutyryl-3(S)-hydroxy-L-aspartyl-4-chloro-L-threonine C-1.9-O-3.1-lactone 【CA登记号】 【 分 子 式 】C72H116ClN13O30 【 分 子 量 】1679.24942 |
【开发单位】Lilly (Originator) 【药理作用】Antifungal Agents, ANTIINFECTIVE THERAPY, Chemical Delivery Systems, DRUG DELIVERY, Drug Delivery Systems |
合成路线1
Acylation of pseudomycin B (I) with the succinimidyl ester (III), prepared from chloroformate (II), produced a mixture of mono-, di- and tri-N-acylated compounds, which were separated by means of HPLC. The required trisubstituted compound (IV) was then condensed with cyclopropylamine (V) in the presence of TBTU to afford the title amide.
| 【1】 Sun, X.; et al.; Prodrugs of 3-amido bearing pseudomycin analogues: Novel antifungal agents. Bioorg Med Chem Lett 2001, 11, 14, 1881. |
| 【2】 Chen, S.H.; Sun, X.D.; Rodriguez, M.J. (Eli Lilly and Company); Pseudomycin prodrugs. WO 0105813 . |
| 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) | 50469 | (2S)-2-((3S,6S,12S,15S,18S,21S,24R,27S)-18-(4-aminobutyl)-15,24-bis(2-aminoethyl)-21-(carboxymethyl)-3-[(1S)-2-chloro-1-hydroxyethyl]-9-[(Z)ethylidene]-12-[(1S)-1-hydroxyethyl]-27-[[(3R)-3-hydroxytetradecanoyl]amino]-2,5,8,11,14,17,20,23,26-nonaoxo-1-oxa-4,7,10,13,16,19,22,25-octaazacyclooctacosan-6-yl)-2-hydroxyethanoic acid | C51H87ClN12O19 | 详情 | 详情 | |
| (II) | 52496 | [(chlorocarbonyl)oxy]methyl 2-methylpropanoate | C6H9ClO4 | 详情 | 详情 | |
| (III) | 52497 | ({[(2,5-dioxo-1-pyrrolidinyl)oxy]carbonyl}oxy)methyl 2-methylpropanoate | C10H13NO7 | 详情 | 详情 | |
| (IV) | 52498 | C69H111ClN12O31 | 详情 | 详情 | ||
| (V) | 12263 | Cyclopropylamine; Cyclopropanamine | 765-30-0 | C3H7N | 详情 | 详情 |