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【结 构 式】 
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【分子编号】19278 【品名】ethyl 2-[[1-((2S)-2-[[(benzyloxy)carbonyl]amino]propanoyl)-4-piperidinyl]oxy]acetate 【CA登记号】 |
【 分 子 式 】C20H28N2O6 【 分 子 量 】392.4522 【元素组成】C 61.21% H 7.19% N 7.14% O 24.46% |
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：(III)1) The condensation of benzyloxycarbonyl-L-alanine (I) with 2-(4-piperidyloxy)acetic acid ethyl ester (II) by means of pivaloyl chloride and triethylamine in ethyl acetate gives the protected alanyl-piperidine (III), which is deprotected by hydrogenation over Pd/C in ethanol to yield compound (IV). The condensation of (IV) with 4-cyanobenzoyl chloride (V) by means of triethylamine in toluene affords the corresponding benzoyl derivative (VI), which is finally treated with hydroxylamine in the same solvent.
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【1】
Castañer, J.; Graul, A.; Merlos, M.; Sibrafiban |
| 【2】 Trussardi, R.; Karpf, M. (F. Hoffmann-La Roche AG); Process for the preparation of mixed anhydrides. EP 0847994 . |
| 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) | 61209 | CBZ-L-Alanine; (2S)-2-[[(Benzyloxy)carbonyl]amino]propionic acid; N-((Phenylmethoxy)carbonyl)-alanine; Carbobenzyloxy-L-alanine | C11H13NO4 | 详情 | 详情 | |
| (II) | 19277 | ethyl 2-(4-piperidinyloxy)acetate | C9H17NO3 | 详情 | 详情 | |
| (III) | 19278 | ethyl 2-[[1-((2S)-2-[[(benzyloxy)carbonyl]amino]propanoyl)-4-piperidinyl]oxy]acetate | C20H28N2O6 | 详情 | 详情 | |
| (IV) | 19279 | ethyl 2-([1-[(2S)-2-aminopropanoyl]-4-piperidinyl]oxy)acetate | C12H22N2O4 | 详情 | 详情 | |
| (V) | 19280 | 4-cyanobenzoyl chloride | 6068-72-0 | C8H4ClNO | 详情 | 详情 |
| (VI) | 19281 | ethyl 2-[(1-[(2S)-2-[(4-cyanobenzoyl)amino]propanoyl]-4-piperidinyl)oxy]acetate | C20H25N3O5 | 详情 | 详情 |
Extended Information