← Back to patent-cliff list
Setmelanotide Acetate
Tier C — Watch / tradeSetmelanotide Acetate
-
Originator
2020
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type
Targets：MC4R
Brand：Imcivree
Indications (approved)：下丘脑肥胖, 巴德特-别德尔综合征, Obesity
Regional status
US
Approved
2020-11-25
EU
Approved
2021-07-16
China
Phase I
2022-08-24
Japan
Approved
2026-08-24
Synthetic routes & intermediates7 routes
Originator routes × 0Optimised (non-patent) × 7Process routes × 0
Routes are ordered originator first, then optimised / process (non-patent) routes; each lists steps, overall yield and the intermediate table (code / CAS / name) — ready for supplier sourcing and RFQ. Rendered by this site from structured data; no third-party route graphics used.
OptimisedRoute 1Steps 5 · Total yield /
(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
| Code | CAS No. | Intermediate |
|---|---|---|
| (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 |
OptimisedRoute 2Steps 3 · Total yield /
(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
| Code | CAS No. | Intermediate |
|---|---|---|
| (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 |
OptimisedRoute 3Steps 2 · Total yield /
(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
| Code | CAS No. | Intermediate |
|---|---|---|
| (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 |
OptimisedRoute 4Steps 4 · Total yield /
(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
| Code | CAS No. | Intermediate |
|---|---|---|
| (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 |
OptimisedRoute 5Steps 2 · Total yield /
(IX)443746-2-b1304512-45-5(VIII)443746-2-a,(VIII)443746-2-b1304512-44-4API · Setmelanotide Acetate
| Code | CAS No. | Intermediate |
|---|---|---|
| (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 |
OptimisedRoute 6Steps 3 · Total yield /
(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
| Code | CAS No. | Intermediate |
|---|---|---|
| (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 |
OptimisedRoute 7Steps 2 · Total yield /
(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
| Code | CAS No. | Intermediate |
|---|---|---|
| (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 |
Frequently asked questions
What are the approved indications of Setmelanotide Acetate?
Approved indications include: 下丘脑肥胖, 巴德特-别德尔综合征, Obesity.
When does the Setmelanotide Acetate patent expire?
No public expiry year is available for Setmelanotide Acetate yet; this page updates once verified.
How many synthesis routes are recorded for Setmelanotide Acetate?
7 synthesis routes are recorded; the shortest is 2 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Setmelanotide Acetate intermediates?
All intermediates in Setmelanotide Acetate routes have CAS profiles — you can submit an RFQ per CAS and it enters the Unibest matching pool.
How do I get a quote for Setmelanotide Acetate intermediates?
Open the CAS profile of the target intermediate from this page, or submit an RFQ directly — the CAS enters the matching flow automatically and the supply network responds with quotes.
Source: cross-verified data (structured fields only) · 2026-09-27