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Last Updated: May 2, 2024

Claims for Patent: 10,953,112

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Summary for Patent: 10,953,112

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:	16/852,910
Patent Claims:	1. A method of using 1-amino-3-[.sup.18F]fluorocyclobutanecarboxylic acid comprising: producing 1-amino-3-[.sup.18F]fluorocyclobutanecarboxylic acid from a precursor compound which is represented by formula (1), ##STR00003## wherein, n is 0; R.sup.1 is ethyl; X is .sup.18F; and R.sup.3 is a t-butoxycarbonyl group, deprotecting the precursor compound to produce 1-amino-3-[.sup.18F]fluorocyclobutanecarboxylic acid, wherein the deprotecting produces ethanol, and wherein the 1-amino-3-[.sup.18F]fluorocyclobutanecarboxylic acid is subsequently administered to a subject in order to carry out Positron Emission Tomography. 2. The method according to claim 1, wherein the precursor compound is anti-[.sup.18F]1-(N-(t-butoxycarbonyl)amino)-3-fluorocyclobutane-1-carbox- ylic acid ethyl ester. 3. The method according to claim 1, wherein the deprotecting comprises acid hydrolysis. 4. The method according to claim 3, wherein the hydrolysis is a reaction in the presence of hydrochloric acid.

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