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【结 构 式】 
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【分子编号】67646 【品名】methyl 1-(hydroxymethyl)cyclopropanecarboxylate 【CA登记号】 |
【 分 子 式 】C6H10O3 【 分 子 量 】130.1436 【元素组成】C 55.37% H 7.74% O 36.88% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(XXVI)Intermediate (XIV) is obtained by selective hydrolysis of dimethyl 1,1-cyclopropanedicarboxylate (XXIII) using NaOH in MeOH/H2O to afford acid-ester (XXIV), which by treatment with ClCO2Et in THF gives the mixed anhydride (XXV). Reduction of carboxylic anhydride (XXV) using NaBH4 in MeOH gives the primary alcohol (XXVI), which is finally activated as mesylate (XIV) by means of MsCl in the presence of DIEA in CH2Cl2 at 0 °C .
| 【1】 Chen, G.P. (Advenchen Laboratories, LLC). Spiro substituted compounds as angiogenesis inhibitors. KR 2015039889; US 8163923; EP 2125777; JP 2010521474; WO 2008112408; US 2008227812. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (XIV) | 67637 | 1-(4-hydroxy-3-methoxyphenyl)ethanone | C7H12O5S | 详情 | 详情 | |
| (XXIII) | 58458 | dimethyl 1,1-cyclopropanedicarboxylate; cyclopropane-1,1-dicarboxylic acid dimethyl ester; 1,1-cyclopropanedicarboxylic acid dimethyl ester | 6914-71-2 | C7H10O4 | 详情 | 详情 |
| (XXIV) | 58459 | 1-(methoxycarbonyl)cyclopropanecarboxylic acid | 113020-21-6 | C6H8O4 | 详情 | 详情 |
| (XXV) | 67645 | (ethyl carbonic) 1-(methoxycarbonyl)cyclopropanecarboxylic anhydride | C9H12O6 | 详情 | 详情 | |
| (XXVI) | 67646 | methyl 1-(hydroxymethyl)cyclopropanecarboxylate | C6H10O3 | 详情 | 详情 |
Extended Information