← Back to patent-cliff list
CAS 137076-54-1
DOTA-Tris(t-Bu)ester
Codes: Lutetium (177Lu) vipivotide tetraxetan-012, (XVIII) 847759-1-c
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 tetraxetanMetastatic breast cancerLutetium (177Lu) zaregreptide dizuxetanBreast cancerLutetium (177Lu) zaregreptide dizuxetanNeoplasmLutetium (177Lu) zaregreptide dizuxetanProstate cancerLutetium (177Lu) zaregreptide dizuxetanNeuroendocrine carcinomaLutetium (177Lu) zaregreptide dizuxetanSolid tumourLutetium (177Lu) zaregreptide dizuxetan
Source drugs (routes using this intermediate)
| Drug | Tier | Expiry |
|---|---|---|
| Lutetium (177Lu) vipivotide tetraxetan | Tier B — Position early | - |
| Lutetium (177Lu) zaregreptide dizuxetan | Tier 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.
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: 1total yield: 286mg(Lutetium (177Lu) vipivotide tetraxetan-013)
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
Lutetium (177Lu) vipivotide tetraxetanOptimised routesteps: 1total yield: 286mg(Lutetium (177Lu) vipivotide tetraxetan-013)
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→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
Resin bound N-([2-oxo-2-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)anilino]ethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine→Resin bound D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine→(2-[4-[([[(9H-Fluoren-9-yl)methoxy]carbonyl]amino)methyl]anilino]-2-oxoethoxy)acetic acid→Resin bound N-([2-[4-(aminomethyl)anilino]-2-oxoethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine→DOTA-Tris(t-Bu)ester
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.