← Back to patent-cliff list

CAS 112883-43-9

Fmoc-2-Nal-OH

Codes: Lutetium (177Lu) vipivotide tetraxetan-008, (IV)755707-1-a

Application context (from source-drug indications)

Hormone-sensitive prostate cancerLutetium (177Lu) vipivotide tetraxetanCastration-resistant prostate cancerLutetium (177Lu) vipivotide tetraxetanProstate cancerLutetium (177Lu) vipivotide tetraxetanLiver cancerLutetium (177Lu) vipivotide tetraxetanHepatocellular carcinomaLutetium (177Lu) vipivotide tetraxetanRenal cell carcinomaLutetium (177Lu) vipivotide tetraxetanCushing's syndrome68Ga-pentixafor醛固酮增多症68Ga-pentixaforSarcoidosis68Ga-pentixaforGraft-versus-host disease68Ga-pentixaforNeuroendocrine tumour68Ga-pentixaforMarginal zone B-cell lymphoma68Ga-pentixafor

Source drugs (routes using this intermediate)

DrugTierExpiry
Lutetium (177Lu) vipivotide tetraxetanTier B — Position early-
68Ga-pentixaforTier C — Watch / trade-

Position in synthesis routes (up/downstream chain)

Ordered by route registration; left → right is the synthesis direction. The highlighted node is the current CAS; others link to their own profiles.

Lutetium (177Lu) vipivotide tetraxetanOptimised routesteps: 8total yield: /
L-Glutamic acid di-tert-butyl ester hydrochloride→L-Glutamic acid di(tert-butyl) ester→Di-tert-butyl 2(S)-isocyanatopentanedioate→Di-tert-butyl N-[(trichloromethoxy)carbonyl]-L-glutamate→Resin bound H-Lys(Alloc)-OH→Resin bound (2S)-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)-6-([[(prop-2-en-1-yl)oxy]carbonyl]amino)hexanoic acid→Resin bound (2S)-6-amino-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid→Fmoc-2-Nal-OH→Resin bound 6-[[(2S)-2-amino-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid→Fmoc-tranexamic acid→Resin bound (2S)-6-[[(2S)-2-[[(1r,4S)-4-(aminomethyl)cyclohexane-1-carbonyl]amino]-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid→DOTA-Tris(t-Bu)ester→(3S,10S,14S)-3-[(Naphthalen-2-yl)methyl]-1,4,12-trioxo-1-[(1r,4S)-4-([2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)cyclohexyl]-2,5,11,13-tetraazahexadecane-10,14,16-tricarboxylic acid→N6-[(Allyloxy)carbonyl]-N2-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-lysine→Resin bound N2-[[(9H-fluoren-9-yl)methoxy]carbonyl]-N6-[[(prop-2-en-1-yl)oxy]carbonyl]-L-lysine
Lutetium (177Lu) vipivotide tetraxetanOptimised routesteps: 5total yield: 176mg(PSMA-617 (Free))
1,1-Bis(1H-imidazol-1-yl)methanone→Di-tert-butyl L-glutamate hydrogen chloride→Di-tert-butyl N-(1H-imidazole-1-carbonyl)-L-glutamate→Resin bound Fmoc-L-Lys(ivDde)→Resin bound N6-[1-(4,4-dimethyl-2,6-dioxocyclohexylidene)-3-methylbutyl]-L-lysine→Resin bound (2S)-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)-6-[[1-(4,4-dimethyl-2,6-dioxocyclohexylidene)-3-methylbutyl]amino]hexanoic acid→Fmoc-2-Nal-OH→Resin bound 6-[[(2S)-2-amino-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid→(1r,4r)-4-[([[(9H-Fluoren-9-yl)methoxy]carbonyl]amino)methyl]cyclohexane-1-carboxylic acid→Resin bound (2S)-6-[[(2S)-2-[[(1r,4S)-4-(aminomethyl)cyclohexane-1-carbonyl]amino]-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid
Lutetium (177Lu) vipivotide tetraxetanOptimised routesteps: 5total yield: 176mg(PSMA-617 (Free))
tert-Butyl N6-[[(9H-fluoren-9-yl)methoxy]carbonyl]-L-lysinate hydrogen chloride→Staab's reagent→tert-Butyl N6-[[(9H-fluoren-9-yl)methoxy]carbonyl]-N2-(1H-imidazole-1-carbonyl)-L-lysinate→Resin bound Fmoc-Glu(t-Bu)→Resin bound (2S)-2-amino-5-tert-butoxy-5-oxopentanoic acid→Resin bound (9S,13S)-9-(tert-butoxycarbonyl)-13-(3-tert-butoxy-3-oxopropyl)-1-(9H-fluoren-9-yl)-3,11-dioxo-2-oxa-4,10,12-triazatetradecan-14-oic acid→Fmoc-2-Nal-OH→Resin bound (2S)-2-([[(2S)-6-[[(2S)-2-amino-3-(naphthalen-2-yl)propanoyl]amino]-1-tert-butoxy-1-oxohexan-2-yl]carbamoyl]amino)-5-tert-butoxy-5-oxopentanoic acid→Fmoc-tranexamic acid→Resin bound [(2S,6S,13S)-15-[(1r,4S)-4-(aminomethyl)cyclohexyl]-6-(tert-butoxycarbonyl)-2-(3-tert-butoxy-3-oxopropyl)-13-[(naphthalen-2-yl)methyl]-4,12,15-trioxo-3,5,11,14-tetraazapentadecanan-1-oyl]oxy
68Ga-pentixaforOptimised routesteps: 7total yield: /
2-(9H-Fluoren-9-ylmethoxycarbonylamino)acetic acid→Resin bound [([[(9H-Fluoren-9-yl)methoxy]carbonyl]amino)acetyl]oxy→Resin bound glycine→Fmoc-2-Nal-OH→TCP resin bound [[2(S)-amino-3-(naphthalen-2-yl)propanoyl]amino]acetic acid→(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→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→N5-(4-Nitrobenzene-1-sulfonyl)-N2-[[(prop-2-en-1-yl)oxy]carbonyl]-D-ornithine→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→Hydroxymethane→(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→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

Intermediates available on this site

No listed intermediates for this target yet — send an RFQ directly and it will enter our matching pool.

This is a CAS-level registry record: registrations across routes are merged. Supplier offers and buyer demands will be matched on this CAS as the primary key.