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US 10,870,649 B2Granted
Synthesis of NIR fluorescent probe
AssigneeBracco Imaging S.P.A.
InventorsLuciano Lattuada, Federica Buonsanti, Federico Crivellin, Fulvio Ferretti, Federico Maisano, Laura Orio, Lorena Pizzuto
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Abstract
The application relates to a process for the synthesis of a Near Infra-Red (NIR) fluorescent probe which is a cRGD-Cy5.5 conjugate of formula (I) known as DA364 comprising an aza-bicycloalkane based cyclic peptide labelled with a Cy5.5 dye moiety and used in the guided surgery of tumors and pathologic regions.
Claims15
A process for the preparation of a cRGD-Cy5.5 conjugate of formula (I)
- which comprises the steps of:
- a) hydrogenating a compound of formula (II)
- wherein Mtr is a 2,3,6-trimethyl-4-methoxybenzene-sulfonyl group, to provide its amino-derivative of formula (III)
- wherein Mtr is as defined above;
- b) reacting, in the presence of a base and a coupling reagent, the compound of formula (III) with a compound of formula (IV)
- to provide a compound of formula (V)
- wherein Mtr is as defined above;
- c) deprotecting the compound of formula (V) to obtain the compound of formula (I).
5 more elements
Dependencies are inferred from the claim text.