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US 2026/0285818 A1Published application
Synthesis of prostate specific membrane antigen (psma) ligands
AssigneeNovartis AG
InventorFritz ANDREAE
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Abstract
The present disclosure relates to the synthesis of prostate specific membrane antigen (PSMA) ligands that are useful in the treatment of diseases like cancer. In particular, the disclosure relates to a method for synthesizing PSMA ligands having a glutamate-urea-lysine (GUL) moiety and a chelating agent that can comprise a radiometal.
Claims7
A trifluoroacetic acid salt of a compound of formula (I):
- obtained by solid phase synthesis, wherein said solid phase synthesis comprises:
- a) coupling 2-(4,7,10-tris(2-(tert-butoxy)-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetic acid to a resin-bound compound, wherein the resin-bound compound is compound [6] or compound [13]
- using (1H-benzotriazol-1-yloxy)tripyrrolidino-phosphonium hexafluorophosphate and N,N-diisopropylethylamine, and
- b) cleaving the resulting resin-based compound using trifluoroacetic acid, water, and triisopropylsilane, thereby providing the trifluoroacetic acid salt of the compound of formula (I).
1 more element
Dependencies are inferred from the claim text.