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Setmelanotide Acetate
Tier C · 观察 / 贸易Setmelanotide Acetate
益普生
原研
2020
首批上市
-
到期年（公开口径）
无销量数据
峰值销售
化学药
类型
靶点：MC4R
商品名：Imcivree
适应症（已批准）：下丘脑肥胖、巴德特-别德尔综合征、肥胖症
各地区研发/上市状态
美国
批准上市
2020-11-25
欧盟
批准上市
2021-07-16
中国
临床一期
2022-08-24
日本
批准上市
2026-08-24
合成路线与中间体7 routes
原研路线 × 0优化路线（非专利）× 7工艺路线 × 0
路线按「原研路线 → 优化路线 / 工艺路线（非专利）」排序。每条路线附本站自绘的路线流程图（中间体 → 原料药）与中间体表（编号 / CAS / 英文名），可直接用于供应商开发与询价。流程图由本站依据已授权的结构化数据自行渲染，未使用任何第三方路线图。
优化Route 1步骤 5 · 总收率 /
(Ia)443746-1-a,(Ia)443746-1-b103213-32-7(Ib)443746-1-a,(Ib)443746-1-b86060-81-3(IIa)443746-1-a—(IIb)443746-1-a—(IIIa)443746-1-a143824-78-6(IIIb)443746-1-a35737-15-6(IVa)443746-1-a—(IVb)443746-1-a—(IVc)443746-1-a—(IX)443746-1-a109425-51-6(V)443746-1-a,(V)443746-1-b154445-77-9(VIa)443746-1-a—(VIb)443746-1-a—(VIc)443746-1-a—(VII)443746-1-a86123-10-6(VIIIa)443746-1-a—(VIIIb)443746-1-a—(VIIIc)443746-1-a—(Xa)443746-1-a,(Xa)443746-1-b—(Xb)443746-1-a,(Xb)443746-1-b—(Xc)443746-1-a,(Xc)443746-1-b—(XIIa)443746-1-b—(XIIIa)443746-1-b—(XIVa)443746-1-b,(XIVa)443746-1-c—(XVIIa)443746-1-c—API · Setmelanotide Acetate
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (Ia)443746-1-a,(Ia)443746-1-b | 103213-32-7 | (2R)-2-({[(9H-Fluoren-9-yl)methoxy]carbonyl}amino)-3-[(triphenylmethyl)sulfanyl]propanoic acid |
| (Ib)443746-1-a,(Ib)443746-1-b | 86060-81-3 | (2R)-3-(Acetamidomethylsulfanyl)-2-(9H-fluoren-9-ylmethoxycarbonylamino)propanoic acid |
| (IIa)443746-1-a | - | Resin bound S-trityl-L-cysteinamide |
| (IIb)443746-1-a | - | Resin bound S-(acetamidomethyl)-L-cysteinamide |
| (IIIa)443746-1-a | 143824-78-6 | (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(1-(tert-butoxycarbonyl)-1H-indol-3-yl)propanoic acid |
| (IIIb)443746-1-a | 35737-15-6 | (2S)-2-({([(9H-Fluoren-9-yl)methyl)oxy]carbonyl}amino)-3-(1H-indol-3-yl)propanoic acid |
| (IVa)443746-1-a | - | Resin bound 1-(tert-butoxycarbonyl)-L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide |
| (IVb)443746-1-a | - | Resin bound L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide |
| (IVc)443746-1-a | - | Resin bound L-tryptophyl-S-(acetamidomethyl)-L-cysteinamide |
| (IX)443746-1-a | 109425-51-6 | Nalpha-Fmoc-N(im)-trityl-L-histidine |
| (V)443746-1-a,(V)443746-1-b | 154445-77-9 | (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 |
| (VIa)443746-1-a | - | 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 |
| (VIb)443746-1-a | - | 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 |
| (VIc)443746-1-a | - | 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 |
| (VII)443746-1-a | 86123-10-6 | (2R)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-3-phenylpropanoic acid |
| (VIIIa)443746-1-a | - | 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 |
| (VIIIb)443746-1-a | - | 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 |
| (VIIIc)443746-1-a | - | 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 |
| (Xa)443746-1-a,(Xa)443746-1-b | - | 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 |
| (Xb)443746-1-a,(Xb)443746-1-b | - | 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 |
| (Xc)443746-1-a,(Xc)443746-1-b | - | 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 |
| (XIIa)443746-1-b | - | 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 |
| (XIIIa)443746-1-b | - | 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 |
| (XIVa)443746-1-b,(XIVa)443746-1-c | - | 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 |
| (XVIIa)443746-1-c | - | 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 |
优化Route 2步骤 3 · 总收率 /
(Ia)443746-1-a,(Ia)443746-1-b103213-32-7(Ib)443746-1-a,(Ib)443746-1-b86060-81-3(IIb)443746-1-a—(IIIb)443746-1-a35737-15-6(IVb)443746-1-a—(V)443746-1-a,(V)443746-1-b154445-77-9(VIb)443746-1-a—(VIIIb)443746-1-a—(Xa)443746-1-a,(Xa)443746-1-b—(Xb)443746-1-a,(Xb)443746-1-b—(Xc)443746-1-a,(Xc)443746-1-b—(XI)443746-1-b79990-15-1(XIIa)443746-1-b—(XIIb)443746-1-b—(XIIc)443746-1-b—(XIIIa)443746-1-b—(XIIIb)443746-1-b—(XIIIc)443746-1-b—(XIVa)443746-1-b,(XIVa)443746-1-c—(XIVb)443746-1-b,(XIVb)443746-1-c—(XIVc)443746-1-b,(XIVc)443746-1-c—(XVIIb)443746-1-c—API · Setmelanotide Acetate
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (Ia)443746-1-a,(Ia)443746-1-b | 103213-32-7 | (2R)-2-({[(9H-Fluoren-9-yl)methoxy]carbonyl}amino)-3-[(triphenylmethyl)sulfanyl]propanoic acid |
| (Ib)443746-1-a,(Ib)443746-1-b | 86060-81-3 | (2R)-3-(Acetamidomethylsulfanyl)-2-(9H-fluoren-9-ylmethoxycarbonylamino)propanoic acid |
| (IIb)443746-1-a | - | Resin bound S-(acetamidomethyl)-L-cysteinamide |
| (IIIb)443746-1-a | 35737-15-6 | (2S)-2-({([(9H-Fluoren-9-yl)methyl)oxy]carbonyl}amino)-3-(1H-indol-3-yl)propanoic acid |
| (IVb)443746-1-a | - | Resin bound L-tryptophyl-S-(triphenylmethyl)-L-cysteinamide |
| (V)443746-1-a,(V)443746-1-b | 154445-77-9 | (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 |
| (VIb)443746-1-a | - | 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 |
| (VIIIb)443746-1-a | - | 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 |
| (Xa)443746-1-a,(Xa)443746-1-b | - | 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 |
| (Xb)443746-1-a,(Xb)443746-1-b | - | 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 |
| (Xc)443746-1-a,(Xc)443746-1-b | - | 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 |
| (XI)443746-1-b | 79990-15-1 | (2R)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)propanoic acid |
| (XIIa)443746-1-b | - | 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 |
| (XIIb)443746-1-b | - | 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 |
| (XIIc)443746-1-b | - | 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 |
| (XIIIa)443746-1-b | - | 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 |
| (XIIIb)443746-1-b | - | 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 |
| (XIIIc)443746-1-b | - | 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 |
| (XIVa)443746-1-b,(XIVa)443746-1-c | - | 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 |
| (XIVb)443746-1-b,(XIVb)443746-1-c | - | 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 |
| (XIVc)443746-1-b,(XIVc)443746-1-c | - | 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 |
| (XVIIb)443746-1-c | - | 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 |
优化Route 3步骤 2 · 总收率 /
(XIVa)443746-1-b,(XIVa)443746-1-c—(XIVb)443746-1-b,(XIVb)443746-1-c—(XIVc)443746-1-b,(XIVc)443746-1-c—(XV)443746-1-c64-19-7(XVI)443746-1-c108-24-7(XVIIa)443746-1-c—(XVIIb)443746-1-c—(XVIIc)443746-1-c—API · Setmelanotide Acetate
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XIVa)443746-1-b,(XIVa)443746-1-c | - | 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 |
| (XIVb)443746-1-b,(XIVb)443746-1-c | - | 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 |
| (XIVc)443746-1-b,(XIVc)443746-1-c | - | 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 |
| (XV)443746-1-c | 64-19-7 | Acetic acid |
| (XVI)443746-1-c | 108-24-7 | Acetic acid acetic anhydride |
| (XVIIa)443746-1-c | - | 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 |
| (XVIIb)443746-1-c | - | 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 |
| (XVIIc)443746-1-c | - | Resin bound [N2-acetyl-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-cysteinyl]nitrilo |
优化Route 4步骤 4 · 总收率 /
(I)443746-2-a1309391-55-6(II)443746-2-a19647-70-2(III)443746-2-a1304512-39-7(IV)443746-2-a,(IV)443746-2-c1304512-38-6(V)443746-2-a1304512-40-0(VI)443746-2-a1304512-41-1(VII)443746-2-a,(VII)443746-2-d1304512-42-2(VIII)443746-2-a,(VIII)443746-2-b1304512-44-4API · Setmelanotide Acetate
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)443746-2-a | 1309391-55-6 | N2-Acetyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithine |
| (II)443746-2-a | 19647-70-2 | S-(Acetamidomethyl)-L-cysteine |
| (III)443746-2-a | 1304512-39-7 | N2-Acetyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-S-(acetamidomethyl)-L-cysteine |
| (IV)443746-2-a,(IV)443746-2-c | 1304512-38-6 | Methyl D-alanyl-L-histidyl-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithinate |
| (V)443746-2-a | 1304512-40-0 | Methyl N2-acetyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-S-(acetamidomethyl)-L-cysteinyl-D-alanyl-L-histidyl-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithinate |
| (VI)443746-2-a | 1304512-41-1 | (6S,9R,12R,15S,18R)-6-Acetamido-9-[[(acetamidomethyl)sulfanyl]methyl]-18-benzyl-N-[(2S)-1-hydrazinyl-1-oxo-5-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]pentan-2-yl]-15-[(1H-imidazol-4-yl)methyl]-1-imino-12-methyl-7,10,13,16-tetraoxo-1-[(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)amino]-2,8,11,14,17-pentaazanonadecan-19-amide |
| (VII)443746-2-a,(VII)443746-2-d | 1304512-42-2 | Methyl L-tryptophyl-S-(acetamidomethyl)-L-cysteinate |
| (VIII)443746-2-a,(VIII)443746-2-b | 1304512-44-4 | Methyl N2-acetyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-S-(acetamidomethyl)-L-cysteinyl-D-alanyl-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-cysteinate |
优化Route 5步骤 2 · 总收率 /
(IX)443746-2-b1304512-45-5(VIII)443746-2-a,(VIII)443746-2-b1304512-44-4API · Setmelanotide Acetate
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (IX)443746-2-b | 1304512-45-5 | N2-Acetyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-S-(acetamidomethyl)-L-cysteinyl-D-alanyl-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 |
| (VIII)443746-2-a,(VIII)443746-2-b | 1304512-44-4 | Methyl N2-acetyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithyl-S-(acetamidomethyl)-L-cysteinyl-D-alanyl-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-cysteinate |
优化Route 6步骤 3 · 总收率 /
(IV)443746-2-a,(IV)443746-2-c1304512-38-6(X)443746-2-c2448-45-5(XI)443746-2-c257288-19-0(XII)443746-2-c1304512-36-4(XIII)443746-2-c1304512-35-3(XIV)443746-2-c4132-86-9(XV)443746-2-c71-00-1(XVI)443746-2-c1304512-37-5API · Setmelanotide Acetate
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (IV)443746-2-a,(IV)443746-2-c | 1304512-38-6 | Methyl D-alanyl-L-histidyl-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithinate |
| (X)443746-2-c | 2448-45-5 | N-[Benzyloxycarbonyl]-D-phenylalanine |
| (XI)443746-2-c | 257288-19-0 | Methyl N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithinate hydrogen chloride |
| (XII)443746-2-c | 1304512-36-4 | Methyl N-[(benzyloxy)carbonyl]-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithinate |
| (XIII)443746-2-c | 1304512-35-3 | N-[(Benzyloxy)carbonyl]-D-alanyl-L-histidine |
| (XIV)443746-2-c | 4132-86-9 | N-(Benzyloxycarbonyl)-D-alanine |
| (XV)443746-2-c | 71-00-1 | (S)-2-Amino-3-(4-imidazolyl)propionic acid |
| (XVI)443746-2-c | 1304512-37-5 | Methyl N-[(benzyloxy)carbonyl]-D-alanyl-L-histidyl-D-phenylalanyl-N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithinate |
优化Route 7步骤 2 · 总收率 /
(VII)443746-2-a,(VII)443746-2-d1304512-42-2(XIX)443746-2-d1304512-43-3(XVII)443746-2-d13139-14-5(XVIII)443746-2-d55300-64-6API · Setmelanotide Acetate
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (VII)443746-2-a,(VII)443746-2-d | 1304512-42-2 | Methyl L-tryptophyl-S-(acetamidomethyl)-L-cysteinate |
| (XIX)443746-2-d | 1304512-43-3 | Methyl N-(tert-butoxycarbonyl)-L-tryptophyl-S-(acetamidomethyl)-L-cysteinate |
| (XVII)443746-2-d | 13139-14-5 | (2S)-3-(1H-Indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoic acid |
| (XVIII)443746-2-d | 55300-64-6 | Methyl S-(acetamidomethyl)-L-cysteinate |
常见问题（FAQ）
Setmelanotide Acetate的适应症有哪些？
已批准的适应症包括：下丘脑肥胖、巴德特-别德尔综合征、肥胖症。
Setmelanotide Acetate的专利什么时候到期？
Setmelanotide Acetate的专利到期年暂无公开口径，本页会在数据管道核实后更新。
Setmelanotide Acetate有几条合成路线？
本站收录 7 条合成路线，最短路线 2 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
Setmelanotide Acetate的关键中间体在哪里可以采购？
Setmelanotide Acetate路线中的中间体均已建立 CAS 档案，可直接按 CAS 发起询价，需求会进入供应网络撮合池。
如何获取Setmelanotide Acetate中间体的报价？
在本页选择目标中间体的 CAS 进入档案页，或在询价页直接提交需求；CAS 会自动带入供需撮合流程，由供应网络反馈报价。
数据来源：多源数据交叉核实（仅结构化字段） · 2026-09-27