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CAS 86060-81-3
(2R)-3-(Acetamidomethylsulfanyl)-2-(9H-fluoren-9-ylmethoxycarbonylamino)propanoic acidS-(Acetamidomethyl)-N-[[(9H-fluoren-9-yl)methoxy]carbonyl]-L-cysteine
登记编号：(Ib)443746-1-a,(Ib)443746-1-b、Atosiban-095
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产科分娩（早产）阿托西班醋酸盐早产（孕37周前）阿托西班醋酸盐子宫内膜异位症阿托西班醋酸盐
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 | - |
| 阿托西班醋酸盐Atosiban acetate | 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
(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-(acetamidomethyl)-L-cysteinamide→(2S)-2-({([(9H-Fluoren-9-yl)methyl)oxy]carbonyl}amino)-3-(1H-indol-3-yl)propanoic acid→Resin bound L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→(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-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 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→(2R)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)propanoic acid→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 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-L-tryptophyl-S-(triphenylmethyl)-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-L-tryptophyl-S-(acetamidomethyl)-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 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-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide→Resin bound S-(acetamidomethyl)-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-L-tryptophyl-S-(acetamidomethyl)-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 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-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-(acetamidomethyl)-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-L-tryptophyl-S-(acetamidomethyl)-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-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide
Resin bound glycine→CTC resin bound N5-(tert-butoxycarbonyl)-L-ornithylglycine→CTC resin bound L-prolyl-N5-(tert-butoxycarbonyl)-L-ornithylglycine→S-(Acetamidomethyl)-N-[[(9H-fluoren-9-yl)methoxy]carbonyl]-L-cysteine→CTC resin bouond S-(triphenylmethyl)-L-cysteinyl-L-prolyl-N5-(tert-butoxycarbonyl)-L-ornithylglycine→CTC resin bound N-(triphenylmethyl)-L-asparaginyl-S-(acetamidomethyl)-L-cysteinyl-L-prolyl-N5-(tert-butoxycarbonyl)-L-ornithylglycine→N-(9H-Fluoren-9-ylmethoxycarbonyl)glycine→N5-(tert-Butoxycarbonyl)-N2-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-ornithine→N-(9-Fluorenylmethoxycarbonyl)-L-proline→Nalpha-(9-Fluorenylmethoxycarbonyl)-Ngamma-trityl-L-asparagine
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