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Last Updated: April 25, 2024

Claims for Patent: 10,010,632


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Summary for Patent: 10,010,632
Title:Precursor compound of radioactive halogen-labeled organic compound
Abstract: 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 [.sup.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: ##STR00001## wherein n is an integer of 0 or of 1 to 4; R.sup.1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by --OR.sup.2; R.sup.2 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 R.sup.3 is a protective group.
Inventor(s): Ito; Osamu (Chiba, JP), Hayashi; Akio (Chiba, JP), Kurosaki; Fumie (Chiba, JP), Toyama; Masahito (Chiba, JP), Shinmura; Toshiyuki (Chiba, JP), Harano; Arinori (Chiba, JP)
Assignee: NIHON MEDI-PHYSICS CO., LTD. (Tokyo, JP)
Application Number:14/872,305
Patent Claims: 1. A diagnostic agent containing 1-amino-3-[.sup.18F]fluorocyclobutanecarboxylic acid and ethanol rather than methanol as an impurity, wherein said 1-amino-3-[.sup.18F]fluorocyclobutanecarboxylic acid is obtained using a precursor compound that substantially gives ethanol rather than methanol in the production of 1-amino-3-[.sup.18F]fluorocyclobutanecarboxylic acid, wherein said precursor compound is represented by the following formula (1): ##STR00003## wherein n is 0; R.sup.1 is an ethyl substitutent; X is a trifluoromethanesulfonic acid substitutent; and R.sup.3 is a t-butoxycarbonyl group.

2. The diagnostic agent according to claim 1, wherein the precursor compound is represented by formula (2): ##STR00004## wherein Et is an ethyl substitutent; TfO is a trifluoromethanesulfonic acid substitutent; and Boc is a t-butoxycarbonyl group.

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