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CAS 3978-80-1

(tert-butoxycarbonyl)-L-tyrosine(S)-2-((tert-butoxycarbonyl)amino)-3-(4-hydroxyphenyl)propanoic acid(2S)-3-(4-Hydroxyphenyl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoic acid

登记编号:GADO-003、YSV-005、(IIIb)1062329-1-a

应用背景(按来源药适应症)

造影检查钆塞酸钠诊断剂钆塞酸钠前列腺癌钆塞酸钠去势抵抗性前列腺肿瘤钆塞酸钠肝癌钆塞酸钠肝细胞癌钆塞酸钠非小细胞肺癌酪丝缬肽

来源药(使用该中间体的合成路线)

品种梯队到期年
钆塞酸钠Gadoxetate DisodiumTier C · 观察 / 贸易-
酪丝缬肽TyroservaltideTier C · 观察 / 贸易-
DazdotuftideTier C · 观察 / 贸易-

合成路线中的位置(上下游链)

按路线登记顺序排列,左→右为合成方向;高亮为当前 CAS,其余可点击跳转对应档案。

酪丝缬肽原研路线步数:5总收率:37 g
Dazdotuftide优化路线步数:5总收率:/
4-Aminophenyl 2-(trimethylammonio)ethyl phosphate→4-Diazoniophenyl 2-(trimethylazaniumyl)ethyl phosphate chloride→(2S)-3-(4-Hydroxyphenyl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoic acid→N-[[(9H-Fluoren-9-yl)methoxy]carbonyl]-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine→N-(tert-Butoxycarbonyl)-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine→Resin bound 3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine→2-(9H-Fluoren-9-ylmethoxycarbonylamino)acetic acid→2-((tert-Butoxycarbonyl)amino)acetic acid→Resin bound glycyl-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine→(2S)-2-{[(9H-Fluoren-9-ylmethoxy)carbonyl]amino}-5-[2-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]pentanoic acid→(2S)-2-{[(tert-Butoxy)carbonyl]amino}-5-{N'-[(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-yl)sulfonyl]carbamimidamido}pentanoic acid→Resin bound N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithylglycyl-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine

本站可供应的对应中间体

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