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68Ga-pentixafor
Tier C — Watch / trade68Ga-pentixafor
Scintomics
Originator
-
First approval
-
Expiry (public)
No sales data
Peak sales
Radiopharmaceutical
Type
Targets：CXCR4
Indications (approved)：Cushing's syndrome, 醛固酮增多症, Sarcoidosis, Graft-versus-host disease, Neuroendocrine tumour, Marginal zone B-cell lymphoma, 中枢神经系统淋巴瘤
Regional status
US
Phase II
2024-09-23
EU
Phase II
2022-10-05
China
-
Japan
-
Synthetic routes & intermediates6 routes
Originator routes × 0Optimised (non-patent) × 6Process 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 7 · Total yield /
(I)755707-1-a29022-11-5(II)755707-1-a—(III)755707-1-a—(IV)755707-1-a112883-43-9(V)755707-1-a—(VI)755707-1-a154445-77-9(VII)755707-1-a—(VIII)755707-1-a,(VIII)755707-1-f—(IX)755707-1-a—(X)755707-1-a67-56-1(XI)755707-1-a—(XII)755707-1-a,(XII)755707-1-b—API · 68Ga-pentixafor
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)755707-1-a | 29022-11-5 | 2-(9H-Fluoren-9-ylmethoxycarbonylamino)acetic acid |
| (II)755707-1-a | - | Resin bound [([[(9H-Fluoren-9-yl)methoxy]carbonyl]amino)acetyl]oxy |
| (III)755707-1-a | - | Resin bound glycine |
| (IV)755707-1-a | 112883-43-9 | Fmoc-2-Nal-OH |
| (V)755707-1-a | - | TCP resin bound [[2(S)-amino-3-(naphthalen-2-yl)propanoyl]amino]acetic acid |
| (VI)755707-1-a | 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 |
| (VII)755707-1-a | - | TCP resin bound [[(2S)-2-([(2S)-2-amino-5-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]pentanoyl]amino)-3-(naphthalen-2-yl)propanoyl]amino]acetic acid |
| (VIII)755707-1-a,(VIII)755707-1-f | - | N5-(4-Nitrobenzene-1-sulfonyl)-N2-[[(prop-2-en-1-yl)oxy]carbonyl]-D-ornithine |
| (IX)755707-1-a | - | TCP resin bound (5S,8S,11R)-5-[(naphthalen-2-yl)methyl]-11-[(4-nitrobenzene-1-sulfonyl)amino]-4,7,10,16-tetraoxo-8-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-17-oxa-3,6,9,15-tetraazaicos-19-en-1-oic acid |
| (X)755707-1-a | 67-56-1Available | Hydroxymethane |
| (XI)755707-1-a | - | (5S,8S,11R)-11-[Methyl(4-nitrobenzene-1-sulfonyl)amino]-5-[(naphthalen-2-yl)methyl]-4,7,10,16-tetraoxo-8-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-17-oxa-3,6,9,15-tetraazaicos-19-en-1-oic acid |
| (XII)755707-1-a,(XII)755707-1-b | - | TCP resin bound (3R,6S,9S)-3-(3-aminopropyl)-9-[(naphthalen-2-yl)methyl]-2-(4-nitrobenzene-1-sulfonyl)-4,7,10-trioxo-6-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-2,5,8,11-tetraazatridecan-13-oic acid |
OptimisedRoute 2Steps 2 · Total yield /
(XII)755707-1-a,(XII)755707-1-b—(XIII)755707-1-b2254340-05-9(XIV)755707-1-b—(XV)755707-1-b,(XV)755707-1-c—API · 68Ga-pentixafor
| Code | CAS No. | Intermediate |
|---|---|---|
| (XII)755707-1-a,(XII)755707-1-b | - | TCP resin bound (3R,6S,9S)-3-(3-aminopropyl)-9-[(naphthalen-2-yl)methyl]-2-(4-nitrobenzene-1-sulfonyl)-4,7,10-trioxo-6-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-2,5,8,11-tetraazatridecan-13-oic acid |
| (XIII)755707-1-b | 2254340-05-9 | 4-([2-[4,7,10-Tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)benzoic acid |
| (XIV)755707-1-b | - | (6R,9S,12S)-6-[Methyl(4-nitrobenzene-1-sulfonyl)amino]-12-[(naphthalen-2-yl)methyl]-1,7,10,13-tetraoxo-9-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-1-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)phenyl]-2,8,11,14-tetraazahexadecan-16-oic acid |
| (XV)755707-1-b,(XV)755707-1-c | - | TCP resin bound (6R,9S,12S)-6-(methylamino)-12-[(naphthalen-2-yl)methyl]-1,7,10,13-tetraoxo-9-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-1-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)phenyl]-2,8,11,14-tetraazahexadecan-16-oic acid |
OptimisedRoute 3Steps 2 · Total yield /
(XV)755707-1-b,(XV)755707-1-c—(XVI)755707-1-c118488-18-9(XVII)755707-1-c—(XVIII)755707-1-c,(XVIII)755707-1-d—API · 68Ga-pentixafor
| Code | CAS No. | Intermediate |
|---|---|---|
| (XV)755707-1-b,(XV)755707-1-c | - | TCP resin bound (6R,9S,12S)-6-(methylamino)-12-[(naphthalen-2-yl)methyl]-1,7,10,13-tetraoxo-9-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-1-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)phenyl]-2,8,11,14-tetraazahexadecan-16-oic acid |
| (XVI)755707-1-c | 118488-18-9 | Fmoc-O-tert-butyl-D-tyrosine |
| (XVII)755707-1-c | - | TCP resin bound (5R,8R,11S,14S)-5-[(4-tert-butoxyphenyl)methyl]-1-(9H-fluoren-9-yl)-7-methyl-14-[(naphthalen-2-yl)methyl]-3,6,9,12,15-pentaoxo-11-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-8-[3-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)benzamido]propyl]-2-oxa-4,7,10,13,16-pentaazaoctadecan-18-oic acid |
| (XVIII)755707-1-c,(XVIII)755707-1-d | - | TCP resin bound (6R,9S,12S)-6-[[(2R)-2-amino-3-(4-tert-butoxyphenyl)propanoyl](methyl)amino]-12-[(naphthalen-2-yl)methyl]-1,7,10,13-tetraoxo-9-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-1-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)phenyl]-2,8,11,14-tetraazahexadecan-16-oic acid |
OptimisedRoute 4Steps 2 · Total yield /
(XIX)755707-1-d1345509-28-5(XVIII)755707-1-c,(XVIII)755707-1-d—(XX)755707-1-d,(XX)755707-1-e—API · 68Ga-pentixafor
| Code | CAS No. | Intermediate |
|---|---|---|
| (XIX)755707-1-d | 1345509-28-5 | (6R,9S,12S)-6-[[(2R)-2-Amino-3-(4-tert-butoxyphenyl)propanoyl](methyl)amino]-12-[(naphthalen-2-yl)methyl]-1,7,10,13-tetraoxo-9-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-1-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)phenyl]-2,8,11,14-tetraazahexadecan-16-oic acid |
| (XVIII)755707-1-c,(XVIII)755707-1-d | - | TCP resin bound (6R,9S,12S)-6-[[(2R)-2-amino-3-(4-tert-butoxyphenyl)propanoyl](methyl)amino]-12-[(naphthalen-2-yl)methyl]-1,7,10,13-tetraoxo-9-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-1-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)phenyl]-2,8,11,14-tetraazahexadecan-16-oic acid |
| (XX)755707-1-d,(XX)755707-1-e | - | Tri-tert-butyl 2,2',2''-[10-[2-([[4-([3-[(2R,5S,8S,14R)-14-[(4-tert-butoxyphenyl)methyl]-1-methyl-8-[(naphthalen-2-yl)methyl]-3,6,9,12,15-pentaoxo-5-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-1,4,7,10,13-pentaazacyclopentadecan-2-yl]propyl]carbamoyl)phenyl]methyl]amino)-2-oxoethyl]-1,4,7,10-tetraazacyclododecane-1,4,7-triyl]triacetate |
OptimisedRoute 5Steps 4 · Total yield /
(XX)755707-1-d,(XX)755707-1-e—(XXI)755707-1-e1341207-62-2API · 68Ga-pentixafor
| Code | CAS No. | Intermediate |
|---|---|---|
| (XX)755707-1-d,(XX)755707-1-e | - | Tri-tert-butyl 2,2',2''-[10-[2-([[4-([3-[(2R,5S,8S,14R)-14-[(4-tert-butoxyphenyl)methyl]-1-methyl-8-[(naphthalen-2-yl)methyl]-3,6,9,12,15-pentaoxo-5-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-1,4,7,10,13-pentaazacyclopentadecan-2-yl]propyl]carbamoyl)phenyl]methyl]amino)-2-oxoethyl]-1,4,7,10-tetraazacyclododecane-1,4,7-triyl]triacetate |
| (XXI)755707-1-e | 1341207-62-2 | 2,2',2''-(10-[2-[([4-[(3-[(2R,5S,8S,14R)-5-(3-Carbamimidamidopropyl)-14-[(4-hydroxyphenyl)methyl]-1-methyl-8-[(naphthalen-2-yl)methyl]-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl]propyl)carbamoyl]phenyl]methyl)amino]-2-oxoethyl]-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid |
OptimisedRoute 6Steps 3 · Total yield /
(VIII)755707-1-a,(VIII)755707-1-f—(XXII)755707-1-f—(XXIII)755707-1-f—(XXIV)755707-1-f—API · 68Ga-pentixafor
| Code | CAS No. | Intermediate |
|---|---|---|
| (VIII)755707-1-a,(VIII)755707-1-f | - | N5-(4-Nitrobenzene-1-sulfonyl)-N2-[[(prop-2-en-1-yl)oxy]carbonyl]-D-ornithine |
| (XXII)755707-1-f | - | Cyclo[N5-(4-nitrobenzene-1-sulfonyl)-L-ornithine] |
| (XXIII)755707-1-f | - | N2-(tert-Butoxycarbonyl)-N5-(4-nitrobenzene-1-sulfonyl)-D-ornithine |
| (XXIV)755707-1-f | - | N5-(4-Nitrobenzene-1-sulfonyl)-D-ornithine |
Frequently asked questions
What are the approved indications of 68Ga-pentixafor?
Approved indications include: Cushing's syndrome, 醛固酮增多症, Sarcoidosis, Graft-versus-host disease, Neuroendocrine tumour, Marginal zone B-cell lymphoma, 中枢神经系统淋巴瘤.
When does the 68Ga-pentixafor patent expire?
No public expiry year is available for 68Ga-pentixafor yet; this page updates once verified.
How many synthesis routes are recorded for 68Ga-pentixafor?
6 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 68Ga-pentixafor intermediates?
1 intermediate CAS of 68Ga-pentixafor are available through the Unibest supply network — see the route tables on this page and request a quote per CAS.
How do I get a quote for 68Ga-pentixafor 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) · 2026-10-05