【结 构 式】 |
【分子编号】43259 【品名】2-[(3S)-3-[((2R)-3-(benzyloxy)-2-[[(2R)-2-[[2-([[(2R,4S)-1-([(2R)-1-[(2S,5S,8S)-5-(4-[[(benzyloxy)carbonyl]amino]butyl)-8-[(tert-butoxycarbonyl)amino]-2-(3-[[imino([[(4-methylphenyl)sulfonyl]oxy]amino)methyl]amino]propyl)-4,7,14-trioxo-16-phenyl-15- 【CA登记号】 |
【 分 子 式 】C90H113N15O22S2 【 分 子 量 】1821.10712 【元素组成】C 59.36% H 6.25% N 11.54% O 19.33% S 3.52% |
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)The peptidic chain is elongated by deprotection with TFA/EDT and coupling of protected amino acid (Boc-Lys(COOCH2Ph)-OH (XXIV)) with BOP/DIEA, providing derivative (XXVI), which is finally deprotected and cleaved by a first treatment with TFA/EDT followed by HF in the presence of anisole (Scheme 28947001d).
【1】 Bedos, P.; Daffix, I.; Amblard, M.; et al.; Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety. J Med Chem 1999, 42, 20, 4185. |
【2】 Amblard, M.; Bedos, P.; Olivier, C.; Daffix, I.; Luccarini, J.M.; Dodey, P.; Pruneau, D.; Paquet, J.L.; Martinez, J.; Synthesis and biological evaluation of bradykinin B1/B2 and selective B1 receptor antagonists. J Med Chem 2000, 43, 12, 2382. |
中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
---|---|---|---|---|---|---|
(XXIV) | 23159 | (2S)-6-[[(benzyloxy)carbonyl]amino]-2-[(tert-butoxycarbonyl)amino]hexanoic acid | C19H28N2O6 | 详情 | 详情 | |
(XXV) | 43258 | 2-[(3S)-3-[((2R)-3-(benzyloxy)-2-[[(2R)-2-[(2-[[((2R,4S)-1-[[(2R)-1-((2S)-2-([(2S)-6-[[(benzyloxy)carbonyl]amino]-2-[(tert-butoxycarbonyl)amino]hexanoyl]amino)-5-[[imino([[(4-methylphenyl)sulfonyl]oxy]amino)methyl]amino]pentanoyl)pyrrolidinyl]carbon | C76H95N13O19S2 | 详情 | 详情 | |
(XXVI) | 43259 | 2-[(3S)-3-[((2R)-3-(benzyloxy)-2-[[(2R)-2-[[2-([[(2R,4S)-1-([(2R)-1-[(2S,5S,8S)-5-(4-[[(benzyloxy)carbonyl]amino]butyl)-8-[(tert-butoxycarbonyl)amino]-2-(3-[[imino([[(4-methylphenyl)sulfonyl]oxy]amino)methyl]amino]propyl)-4,7,14-trioxo-16-phenyl-15- | C90H113N15O22S2 | 详情 | 详情 |
Extended Information