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CAS 71989-26-9
(S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-6-((tert-butoxycarbonyl)amino)hexanoic acid(2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-6-[(2-methylpropan-2-yl)oxycarbonylamino]hexanoic acid
登记编号：EPTI-011、(XVIII)819152-1-c、SINA-006、(XIIa)1062329-1-b
应用背景（按来源药适应症）
不稳定型心绞痛依替巴肽心肌梗塞依替巴肽缺血性卒中依替巴肽急性冠脉综合征依替巴肽镰状细胞血症依替巴肽ST段抬高型心肌梗死依替巴肽头颈部鳞状细胞癌cRGD-ZW800-1胆管上皮癌cRGD-ZW800-1胰腺癌cRGD-ZW800-1成人呼吸窘迫综合征Sinapultide新型冠状病毒感染Sinapultide新生儿呼吸窘迫综合征Sinapultide
来源药（使用该中间体的合成路线）
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 依替巴肽Eptifibatide | Tier C · 观察 / 贸易 | - |
| cRGD-ZW800-1 | Tier C · 观察 / 贸易 | - |
| Sinapultide | Tier C · 观察 / 贸易 | - |
| Dazdotuftide | Tier 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。
(7S,13S)-tert-butyl 13-(((S)-1-((S)-2-(((R)-1-amino-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)carbamoyl)-7-(4-aminobutyl)-5,8,11-trioxo-1,1,1-triphenyl-2-thia-6,9,12-triazapentadecan-15-oate→3,5-dimethyl-1H-pyrazole-1-carboximidamide→N-(((9H-fluoren-9-yl)methoxy)carbonyl)-S-trityl-L-cysteine→(9H-fluoren-9-yl)methyl (R)-(1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamate→(((9H-fluoren-9-yl)methoxy)carbonyl)-L-proline→(9H-fluoren-9-yl)methyl (S)-2-(((R)-1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidine-1-carboxylate→Na-(((9H-fluoren-9-yl)methoxy)carbonyl)-1-(tert-butoxycarbonyl)-L-tryptophan→(9H-fluoren-9-yl)methyl ((S)-3-(1H-indol-3-yl)-1-((S)-2-(((R)-1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-1-oxopropan-2-yl)carbamate→(S)-tert-butyl 4-(((S)-3-(1H-indol-3-yl)-1-((S)-2-(((R)-1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-1-oxopropan-2-yl)amino)-3-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-4-oxobutanoate→(((9H-fluoren-9-yl)methoxy)carbonyl)glycine→(S)-tert-butyl 4-(((S)-3-(1H-indol-3-yl)-1-((S)-2-(((R)-1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-1-oxopropan-2-yl)amino)-3-(2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)acetamido)-4-oxobutanoate→(S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-6-((tert-butoxycarbonyl)amino)hexanoic acid→(S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-4-(tert-butoxy)-4-oxobutanoic acid→(10S,16S)-tert-butyl 16-(((S)-3-(1H-indol-3-yl)-1-((S)-2-(((R)-1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-1-oxopropan-2-yl)carbamoyl)-10-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-2,2-dimethyl-4,11,14-trioxo-3-oxa-5,12,15-triazaoctadecan-18-oate→3-(tritylthio)propanoic acid
Resin bound [([[(9H-Fluoren-9-yl)methoxy]carbonyl]amino)acetyl]oxy→Resin bound N-[(2S)-2-[[N6-(tert-butoxycarbonyl)-L-lysyl]oxy]-5-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]pentanoyl]glycine→Resin bound glycine→(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→Resin bound N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithylglycine→(2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-6-[(2-methylpropan-2-yl)oxycarbonylamino]hexanoic acid→Fmoc-O-tert-butyl-D-tyrosine→Resin bound (2S)-1-[(carboxymethyl)amino]-1-oxo-5-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]pentan-2-yl O-tert-butyl-D-tyrosyl-N6-(tert-butoxycarbonyl)-L-lysinate→(2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-4-[(2-methylpropan-2-yl)oxy]-4-oxobutanoic acid→Resin bound (5S,8S,11R,14S)-14-amino-8-[4-[(tert-butoxycarbonyl)amino]butyl]-11-[(4-tert-butoxyphenyl)methyl]-18,18-dimethyl-4,7,10,13,16-pentaoxo-5-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-6,17-dioxa-3,9,12-triazanonadecan-1-oic acid
(((9H-fluoren-9-yl)methoxy)carbonyl)-L-leucine→methyl (((9H-fluoren-9-yl)methoxy)carbonyl)-L-leucinate→methyl (((9H-fluoren-9-yl)methoxy)carbonyl)-L-leucyl-L-leucinate→methyl (((9H-fluoren-9-yl)methoxy)carbonyl)-L-leucyl-L-leucyl-L-leucinate→methyl (((9H-fluoren-9-yl)methoxy)carbonyl)-L-leucyl-L-leucyl-L-leucyl-L-leucinate→(S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-6-((tert-butoxycarbonyl)amino)hexanoic acid→methyl N2-(((9H-fluoren-9-yl)methoxy)carbonyl)-N6-(tert-butoxycarbonyl)-L-lysyl-L-leucyl-L-leucyl-L-leucyl-L-leucinate→N2-(((9H-fluoren-9-yl)methoxy)carbonyl)-N6-(tert-butoxycarbonyl)-L-lysyl-L-leucyl-L-leucyl-L-leucyl-L-leucine→methyl N6-(tert-butoxycarbonyl)-N2-N6-(tert-butoxycarbonyl)-L-lysyl-L-leucyl-L-leucyl-L-leucyl-L-leucyl-L-lysinate→methyl N6-(tert-butoxycarbonyl)-N2-N6-(tert-butoxycarbonyl)-N2-N6-(tert-butoxycarbonyl)-L-lysyl-L-leucyl-L-leucyl-L-leucyl-L-leucyl-L-lysyl-L-leucyl-L-leucyl-L-leucyl-L-leucyl-L-lysinate→SINA-011→SINA-012
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→(2S)-1-{[(9H-Fluoren-9-yl)methoxy]carbonyl}pyrrolidine-2-carboxylic acid→(2S)-1-[(2-Methylpropan-2-yl)oxycarbonyl]pyrrolidine-2-carboxylic acid→Resin bound [(2S)-3-(4-hydroxy-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]phenyl)-2-([L-prolyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithylglycyl]amino)propanoyl]oxy→(2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-6-[(2-methylpropan-2-yl)oxycarbonylamino]hexanoic acid→(2S)-2,6-Bis({[(tert-butoxy)carbonyl]amino})hexanoic acid→Resin bound [(2S)-2-([N6-(tert-butoxycarbonyl)-L-lysyl-L-prolyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithylglycyl]amino)-3-(4-hydroxy-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]phenyl)propanoyl]oxy→O-tert-Butyl-N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-threonine→N-(tert-Butoxycarbonyl)-O-tert-butyl-L-threonine→Resin bound [(2S)-2-([O-tert-butyl-L-threonyl-N6-(tert-butoxycarbonyl)-L-lysyl-L-prolyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithylglycyl]amino)-3-(4-hydroxy-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]phenyl)propanoyl]oxy→L-Threonyl-L-lysyl-L-prolyl-L-arginylglycyl-3-[(E)-[4-([[2-(trimethylazaniumyl)ethoxy]phosphinato]oxy)phenyl]diazenyl]-L-tyrosine--trifluoroacetic acid (1/1)
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