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【结 构 式】 
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【分子编号】52113 【品名】(2R,3S)-3-[formyl(tetrahydro-2H-pyran-2-yloxy)amino]-2-isobutyl-4-methyl-N-[(1S,2S)-2-methyl-1-[(2-pyridinylamino)carbonyl]butyl]pentanamide 【CA登记号】 |
【 分 子 式 】C27H44N4O5 【 分 子 量 】504.67032 【元素组成】C 64.26% H 8.79% N 11.1% O 15.85% |
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：(XVI)N-Boc-L-isoleucine (XII) was coupled to 2-aminopyridine (XIII) via activation with carbonyldiimidazole to give the corresponding amide (XIV). Subsequent acidic cleavage of the Boc protecting group of (XIV) afforded the amino amide (XV), which was further coupled with the intermediate acid (XI), yielding the dipeptide derivative (XVI). The tetrahydropyranyl group of (XVI) was finally removed by hydrolysis with 80% acetic acid.
| 【1】 Chan, J.H.; Bubacz, D.G.; Andersen, M.W.; McDougald, D.L.; Stanford, J.B.; Andrews, R.C.; Gaul, M.D.; Rabinowitz, M.H.; Musso, D.L.; Cowan, D.J.; Wiethe, R.W. (GlaxoSmithKline plc); Reverse hydroxamate derivs. as metalloprotease inhibitors. EP 1019386; JP 2001513767; WO 9838179 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (XI) | 52110 | (2R,3S)-3-[formyl(tetrahydro-2H-pyran-2-yloxy)amino]-2-isobutyl-4-methylpentanoic acid | C16H29NO5 | 详情 | 详情 | |
| (XII) | 30009 | (2S,3S)-2-[(tert-butoxycarbonyl)amino]-3-methylpentanoic acid | 13139-16-7 | C11H21NO4 | 详情 | 详情 |
| (XIII) | 11305 | 2-Pyridinamine; 2-Pyridinylamine; 2-Aminopyridine | 504-29-0 | C5H6N2 | 详情 | 详情 |
| (XIV) | 52111 | tert-butyl (1S,2S)-2-methyl-1-[(2-pyridinylamino)carbonyl]butylcarbamate | C16H25N3O3 | 详情 | 详情 | |
| (XV) | 52112 | (2S,3S)-2-amino-3-methyl-N-(2-pyridinyl)pentanamide | C11H17N3O | 详情 | 详情 | |
| (XVI) | 52113 | (2R,3S)-3-[formyl(tetrahydro-2H-pyran-2-yloxy)amino]-2-isobutyl-4-methyl-N-[(1S,2S)-2-methyl-1-[(2-pyridinylamino)carbonyl]butyl]pentanamide | C27H44N4O5 | 详情 | 详情 |
Extended Information