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CAS 530-62-1
1-[(1H-Imidazol-1-yl)carbonyl]1H-imidazole1,1-Bis(1H-imidazol-1-yl)methanoneStaab's reagent
登记编号：(XIV)101438-13-b、(VII)145089-1-a、Lutetium (177Lu) vipivotide tetraxetan-019
应用背景（按来源药适应症）
乳腺癌Paclitaxel/Encequidar mesylate腺癌Paclitaxel/Encequidar mesylate血管肉瘤Paclitaxel/Encequidar mesylate实体瘤Paclitaxel/Encequidar mesylate胰腺癌紫杉醇非小细胞肺癌紫杉醇霍奇金病紫杉醇精原细胞瘤紫杉醇卵巢癌紫杉醇乳腺癌紫杉醇阿尔茨海默病重酒石酸卡巴拉汀痴呆重酒石酸卡巴拉汀帕金森病重酒石酸卡巴拉汀抗胆碱能综合征重酒石酸卡巴拉汀神经行为学表现重酒石酸卡巴拉汀认知障碍重酒石酸卡巴拉汀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 |
|---|---|---|
| Paclitaxel/Encequidar mesylate | Tier C · 观察 / 贸易 | - |
| 紫杉醇Paclitaxel | Tier B · 提前布局 | - |
| 重酒石酸卡巴拉汀Rivastigmine Tartrate | Tier B · 提前布局 | - |
| 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。
(2alpha,5beta,7beta,10beta)-1,2,7,10-Tetrahydroxytaxa-4(20),11-dien-5-yl acetate→1-[(1H-Imidazol-1-yl)carbonyl]1H-imidazole→(3aS,9aS,10S,12R,13S,13aR,13bS)-12,13-Dihydroxy-13-(hydroxymethyl)-6,9a,14,14-tetramethyl-10-[(triethylsilyl)oxy]-9,9a,10,11,12,13,13a,13b-octahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxole-2,8(5H)-dione→(3aS,8S,9aS,10S,12R,13aR,13bS)-8,10-Dihydroxy-6,9a,14,14-tetramethyl-13-methylene-2-oxo-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-12-yl acetate→(3aS,8S,9aS,10S,12R,13aR,13bS)-8-Hydroxy-6,9a,14,14-tetramethyl-13-methylene-2-oxo-10-[(triethylsilyl)oxy]-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-12-yl acetate→(3aS,9aS,10S,12R,13aR,13bS)-6,9a,14,14-Tetramethyl-13-methylene-2,8-dioxo-10-[(triethylsilyl)oxy]-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-12-yl acetate→(3aS,9aS,10S,12S,13aR,13bS)-12-Hydroxy-6,9a,14,14-tetramethyl-13-methylene-10-[(triethylsilyl)oxy]-9,9a,10,11,12,13,13a,13b-octahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxole-2,8(5H)-dione→[(3aS,9aS,10S,12R,13S,13aR,13bS)-12,13-Dihydroxy-6,9a,14,14-tetramethyl-2,8-dioxo-10-[(triethylsilyl)oxy]-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-13-yl]methyl acetate→[(3aS,9aS,10S,12R,13S,13aR,13bS)-13-Hydroxy-6,9a,14,14-tetramethyl-12-[(methylsulfonyl)oxy]-2,8-dioxo-10-[(triethylsilyl)oxy]-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-13-yl]methyl acetate→(3aS,9aS,10S,12S,13S,13aR,13bS)-13-Hydroxy-13-(hydroxymethyl)-6,9a,14,14-tetramethyl-2,8-dioxo-10-[(triethylsilyl)oxy]-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-12-yl methanesulfonate→(3aS,9aS,10S,11aR,13aS,13bR,13cS)-13a-Hydroxy-6,9a,14,14-tetramethyl-10-[(triethylsilyl)oxy]-4,5,9a,10,11,11a,13,13a,13b,13c-decahydro-3a,7-methano[1,3]dioxolo[9,10]cyclodeca[1,2-d][1]benzoxete-2,8(9H)-dione
(2alpha,5beta,7beta,10beta)-1,2,7,10-Tetrahydroxytaxa-4(20),11-dien-5-yl acetate→1-[(1H-Imidazol-1-yl)carbonyl]1H-imidazole→(3aS,9aS,10S,12R,13S,13aR,13bS)-12,13-Dihydroxy-13-(hydroxymethyl)-6,9a,14,14-tetramethyl-10-[(triethylsilyl)oxy]-9,9a,10,11,12,13,13a,13b-octahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxole-2,8(5H)-dione→(3aS,8S,9aS,10S,12R,13aR,13bS)-8,10-Dihydroxy-6,9a,14,14-tetramethyl-13-methylene-2-oxo-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-12-yl acetate→(3aS,8S,9aS,10S,12R,13aR,13bS)-8-Hydroxy-6,9a,14,14-tetramethyl-13-methylene-2-oxo-10-[(triethylsilyl)oxy]-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-12-yl acetate→(3aS,9aS,10S,12R,13aR,13bS)-6,9a,14,14-Tetramethyl-13-methylene-2,8-dioxo-10-[(triethylsilyl)oxy]-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-12-yl acetate→(3aS,9aS,10S,12S,13aR,13bS)-12-Hydroxy-6,9a,14,14-tetramethyl-13-methylene-10-[(triethylsilyl)oxy]-9,9a,10,11,12,13,13a,13b-octahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxole-2,8(5H)-dione→[(3aS,9aS,10S,12R,13S,13aR,13bS)-12,13-Dihydroxy-6,9a,14,14-tetramethyl-2,8-dioxo-10-[(triethylsilyl)oxy]-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-13-yl]methyl acetate→[(3aS,9aS,10S,12R,13S,13aR,13bS)-13-Hydroxy-6,9a,14,14-tetramethyl-12-[(methylsulfonyl)oxy]-2,8-dioxo-10-[(triethylsilyl)oxy]-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-13-yl]methyl acetate→(3aS,9aS,10S,12S,13S,13aR,13bS)-13-Hydroxy-13-(hydroxymethyl)-6,9a,14,14-tetramethyl-2,8-dioxo-10-[(triethylsilyl)oxy]-5,8,9,9a,10,11,12,13,13a,13b-decahydro-4H-3a,7-methanobenzo[3,4]cyclodeca[1,2-d][1,3]dioxol-12-yl methanesulfonate→(3aS,9aS,10S,11aR,13aS,13bR,13cS)-13a-Hydroxy-6,9a,14,14-tetramethyl-10-[(triethylsilyl)oxy]-4,5,9a,10,11,11a,13,13a,13b,13c-decahydro-3a,7-methano[1,3]dioxolo[9,10]cyclodeca[1,2-d][1]benzoxete-2,8(9H)-dione
1-(3-Hydroxyphenyl)ethanone→3-(1-Aminoethyl)phenol→3-[1-(Dimethylamino)ethyl]phenol→N-Ethyl-N-methylcarbamic chloride→N-Ethyl-N-methylcarbamic acid 3-[1-(N,N-dimethylamino)ethyl]phenyl ester→Formic acid N-methylmethanamine→1-[(1H-Imidazol-1-yl)carbonyl]1H-imidazole→N-Ethyl-N-methylamine→(S)-3-(1-(Dimethylamino)ethyl)phenyl ethyl(methyl)carbamate
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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