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CAS 112883-43-9
Fmoc-2-Nal-OH
登记编号：Lutetium (177Lu) vipivotide tetraxetan-008
应用背景（按来源药适应症）
激素敏感性前列腺肿瘤镥[177Lu] 特昔维匹肽去势抵抗性前列腺肿瘤镥[177Lu] 特昔维匹肽前列腺癌镥[177Lu] 特昔维匹肽肝癌镥[177Lu] 特昔维匹肽肝细胞癌镥[177Lu] 特昔维匹肽肾细胞癌镥[177Lu] 特昔维匹肽
来源药（使用该中间体的合成路线）
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 镥[177Lu] 特昔维匹肽Lutetium (177Lu) vipivotide tetraxetan | Tier B · 提前布局 | - |
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。
L-Glutamic acid di-tert-butyl ester hydrochloride→L-Glutamic acid di(tert-butyl) ester→Di-tert-butyl 2(S)-isocyanatopentanedioate→Di-tert-butyl N-[(trichloromethoxy)carbonyl]-L-glutamate→Resin bound H-Lys(Alloc)-OH→Resin bound (2S)-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)-6-([[(prop-2-en-1-yl)oxy]carbonyl]amino)hexanoic acid→Resin bound (2S)-6-amino-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid→Fmoc-2-Nal-OH→Resin bound 6-[[(2S)-2-amino-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid→Fmoc-tranexamic acid→Resin bound (2S)-6-[[(2S)-2-[[(1r,4S)-4-(aminomethyl)cyclohexane-1-carbonyl]amino]-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid→DOTA-Tris(t-Bu)ester→(3S,10S,14S)-3-[(Naphthalen-2-yl)methyl]-1,4,12-trioxo-1-[(1r,4S)-4-([2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)cyclohexyl]-2,5,11,13-tetraazahexadecane-10,14,16-tricarboxylic acid→N6-[(Allyloxy)carbonyl]-N2-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-lysine→Resin bound N2-[[(9H-fluoren-9-yl)methoxy]carbonyl]-N6-[[(prop-2-en-1-yl)oxy]carbonyl]-L-lysine
1,1-Bis(1H-imidazol-1-yl)methanone→Di-tert-butyl L-glutamate hydrogen chloride→Di-tert-butyl N-(1H-imidazole-1-carbonyl)-L-glutamate→Resin bound Fmoc-L-Lys(ivDde)→Resin bound N6-[1-(4,4-dimethyl-2,6-dioxocyclohexylidene)-3-methylbutyl]-L-lysine→Resin bound (2S)-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)-6-[[1-(4,4-dimethyl-2,6-dioxocyclohexylidene)-3-methylbutyl]amino]hexanoic acid→Fmoc-2-Nal-OH→Resin bound 6-[[(2S)-2-amino-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid→(1r,4r)-4-[([[(9H-Fluoren-9-yl)methoxy]carbonyl]amino)methyl]cyclohexane-1-carboxylic acid→Resin bound (2S)-6-[[(2S)-2-[[(1r,4S)-4-(aminomethyl)cyclohexane-1-carbonyl]amino]-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid
tert-Butyl N6-[[(9H-fluoren-9-yl)methoxy]carbonyl]-L-lysinate hydrogen chloride→Staab's reagent→tert-Butyl N6-[[(9H-fluoren-9-yl)methoxy]carbonyl]-N2-(1H-imidazole-1-carbonyl)-L-lysinate→Resin bound Fmoc-Glu(t-Bu)→Resin bound (2S)-2-amino-5-tert-butoxy-5-oxopentanoic acid→Resin bound (9S,13S)-9-(tert-butoxycarbonyl)-13-(3-tert-butoxy-3-oxopropyl)-1-(9H-fluoren-9-yl)-3,11-dioxo-2-oxa-4,10,12-triazatetradecan-14-oic acid→Fmoc-2-Nal-OH→Resin bound (2S)-2-([[(2S)-6-[[(2S)-2-amino-3-(naphthalen-2-yl)propanoyl]amino]-1-tert-butoxy-1-oxohexan-2-yl]carbamoyl]amino)-5-tert-butoxy-5-oxopentanoic acid→Fmoc-tranexamic acid→Resin bound [(2S,6S,13S)-15-[(1r,4S)-4-(aminomethyl)cyclohexyl]-6-(tert-butoxycarbonyl)-2-(3-tert-butoxy-3-oxopropyl)-13-[(naphthalen-2-yl)methyl]-4,12,15-trioxo-3,5,11,14-tetraazapentadecanan-1-oyl]oxy
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