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CAS 143824-78-6
(S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(1-(tert-butoxycarbonyl)-1H-indol-3-yl)propanoic acidNa-(((9H-fluoren-9-yl)methoxy)carbonyl)-1-(tert-butoxycarbonyl)-L-tryptophan
登记编号：(IIIa)443746-1-a、EPTI-005
应用背景（按来源药适应症）
下丘脑肥胖Setmelanotide Acetate巴德特-别德尔综合征Setmelanotide Acetate肥胖症Setmelanotide AcetatePrader-Willi综合征Setmelanotide Acetate垂体疾病Setmelanotide Acetate联合性垂体激素缺乏症Setmelanotide Acetate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
来源药（使用该中间体的合成路线）
| 品种 | 梯队 | 到期年 |
|---|---|---|
| Setmelanotide Acetate | Tier C · 观察 / 贸易 | - |
| 依替巴肽Eptifibatide | 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。
(2R)-2-({[(9H-Fluoren-9-yl)methoxy]carbonyl}amino)-3-[(triphenylmethyl)sulfanyl]propanoic acid→(2R)-3-(Acetamidomethylsulfanyl)-2-(9H-fluoren-9-ylmethoxycarbonylamino)propanoic acid→Resin bound S-trityl-L-cysteinamide→Resin bound S-(acetamidomethyl)-L-cysteinamide→(S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(1-(tert-butoxycarbonyl)-1H-indol-3-yl)propanoic acid→(2S)-2-({([(9H-Fluoren-9-yl)methyl)oxy]carbonyl}amino)-3-(1H-indol-3-yl)propanoic acid→Resin bound 1-(tert-butoxycarbonyl)-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound L-tryptophyl-S-(acetamidomethyl)-L-cysteinamide→Nalpha-Fmoc-N(im)-trityl-L-histidine→(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-ornithyl-1-(tert-butoxycarbonyl)-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-L-tryptophyl-S-(acetamidomethyl)-L-cysteinamide→(2R)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-3-phenylpropanoic acid→Resin bound D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-1-(tert-butoxycarbonyl)-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-L-tryptophyl-S-(acetamidomethyl)-L-cysteinamide→Resin bound 1-(triphenylmethyl)-L-histidyl-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-1-(tert-butoxycarbonyl)-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound 1-(triphenylmethyl)-L-histidyl-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound 1-(triphenylmethyl)-L-histidyl-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-L-tryptophyl-S-(acetamidomethyl)-L-cysteinamide→Resin bound D-alanyl-1-(triphenylmethyl)-L-histidyl-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-1-(tert-butoxycarbonyl)-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound S-(triphenylmethyl)-L-cysteinyl-D-alanyl-1-(triphenylmethyl)-L-histidyl-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-1-(tert-butoxycarbonyl)-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-S-(triphenylmethyl)-L-cysteinyl-D-alanyl-1-(triphenylmethyl)-L-histidyl-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-1-(tert-butoxycarbonyl)-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound N2-acetyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-S-(triphenylmethyl)-L-cysteinyl-D-alanyl-1-(triphenylmethyl)-L-histidyl-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-1-(tert-butoxycarbonyl)-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide
(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
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