Precursor compound of radioactive halogen labeled organic...

Details Precursor compound of radioactive halogen labeled organic... Precursor compound of radioactive halogen labeled organic...

C - Chemistry, Metallurgy

07

C

C07C 309/65 (2006.01) A61K 49/00 (2006.01) C07B 59/00 (2006.01)

Patent

CA 2629227

[PROBLEMS] To provide a novel amino acid organic compound that can be used as a labeled precursor compound of [18F]FACBC and other radioactive halogen labeled amino acid compounds, and that ensures freedom from methanol residue in the produced radioactive halogen labeled amino acid compound. [MEANS FOR SOLVING PROBLEMS] Compounds of the formula: (1) wherein n is 0 or an integer of 1 to 4; R1 is an ethyl substituent, 1-propyl substituent or isopropyl substituent; X is a halogen substituent or group of the formula -OR2 in which R2 is a linear or branched-chain C1-C10 haloalkylsulfonate substituent, C3-C12 trialkylstannyl substituent, fluorosulfonate substituent or aromatic sulfonate substituent; and R3 is a protective group.

L'invention concerne un nouveau composé organique d'acides aminés qui peut être utilisé comme composé précurseur marqué du [18F]FACBC et d'autres composés d'acides aminés marqués à l'halogène radioactif, et qui est dépourvu de résidus méthanol. L'invention se rapporte à des composés de la formule (1) dans laquelle n est 0 ou un entier de 1 à 4; R1 est un substituant éthyle, un substituant 1-propyle ou un substituant isopropyle; X est un substituant halogène ou un groupe de la formule OR2 dans laquelle R2 est un substituant haloalkylsulfonate C1-C10, un substituant trialkylstannyle C3-C12, un substituant fluorosulfonate ou un substituant sulfonate aromatique à chaîne linéaire ou ramifiée; et R3 est un groupe protecteur.

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