Unnatural amino acid radiolabeling precursor

摘要

It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula:;
wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.

主权项

1. A precursor compound for a radioactive halogen-labeled organic compound, which is represented by the following formula (1):wherein
the radioactive halogen-labeled organic compound is 1-amino-3-[18F]fluorocyclobutanecarboxylic acid; n is 0; R1 is an ethyl substituent; X is a trifluoromethanesulfonic acid substituent; R3 is a t-butoxycarbonyl group; and the precursor compound substantially does not give methanol in the production of 1-amino-3-[18F]fluorocyclobutanecarboxylic acid from the precursor compound.