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Details for Patent: 8,758,724

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Details for Patent: 8,758,724

Title:Unnatural amino acid radiolabeling precursor
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 (Sodegaura, JP), Hayashi; Akio (Sodegaura, JP), Kurosaki; Fumie (Sodegaura, JP), Toyama; Masahito (Sodegaura, JP), Shinmura; Toshiyuki (Sodegaura, JP), Harano; Arinori (Sodegaura, JP)
Assignee: Nihon Medi-Physics Co., Ltd. (Tokyo, JP)
Filing Date:Nov 28, 2006
Application Number:12/085,679
Claims:1. A precursor compound for a radioactive halogen-labeled organic compound, which is represented by the following formula (1): ##STR00003## wherein the radioactive halogen-labeled organic compound is 1-amino-3-[.sup.18F]fluorocyclobutanecarboxylic acid; n is 0; R.sup.1 is an ethyl substituent; X is a trifluoromethanesulfonic acid substituent; R.sup.3 is a t-butoxycarbonyl group; and the precursor compound substantially does not give methanol in the production of 1-amino-3-[.sup.18F]fluorocyclobutanecarboxylic acid from the precursor compound.

2. A precursor compound for a radioactive halogen-labeled organic compound, which is represented by the following formula (2): ##STR00004## wherein the radioactive halogen-labeled organic compound is anti-1-amino-3-[.sup.18F]fluorocyclobutanecarboxylic acid; Et is an ethyl substituent; TfO is a trifluoromethanesulfonic acid substituent; Boc is a t-butoxycarbonyl group; and the precursor compound substantially does not give methanol in the production of anti-1-amino-3-[.sup.18F]fluorocyclobutanecarboxylic acid from the precursor compound.
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