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【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
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