放射性ハロゲン標識有機化合物の前駆体化合物の製造方法

Japanese Patent JP5518337

B2

A process for producing a labeled precursor which is useful for production of a radioactive fluorine-labeled amino acid compound is provided. In the reaction step for introducing a leaving group to a mixture of syn-form and anti-form of FACBC, a base is allowed to present in the reaction system to produce a syn-leaving group adduct which is unreactive with the base and is highly stable and an anti-leaving group adduct which can react with the base to form a water-soluble compound. By employing a purification method utilizing such a difference in solubility, the syn-leaving group adduct can be separated selectively. The base may be a linear-chain or branched-chain primary to tertiary alkylamine having 1 to 10 carbon atoms, a nitrogen-containing heterocyclic compound with 2 to 20 carbon atoms, and a nitrogen-containing hetero aromatic compound with 2 to 20 carbon atoms.

Masato Toyama
Akio Hayashi

JP2008551038A

June 11, 2014

December 17, 2007

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Nihon Medi-Physics Co., Ltd.

C07C303/28; C07C303/44; C07C309/65; C07B57/00; C07B59/00

JP2000500442A	2000-01-18
JP2006510706A	2006-03-30

WO2006126410A1

2006-11-30

JPN5005013395; ＬＡＵＲＥＮＴ　ＭＡＲＴＡＲＥＬＬＯ: Ｊ．　ＭＥＤ．　ＣＨＥＭ． Ｖ４５, 20020426, Ｐ２２５０-２２５９
JPN6012014448; Ａｐｐｌｉｅｄ　Ｒａｄｉａｔｉｏｎ　ａｎｄ　Ｉｓｏｔｏｐｅｓ ５８（６）, 2003, ｐ．６５７-６６６
JPN6012066735; Ｌｉｊｕａｎ　Ｊ．　Ｗａｎｇ　ｅｔ　ａｌ: Ｈｅｔｅｒｏａｔｏｍ　Ｃｈｅｍｉｓｔｒｙ Ｖｏｌ．１３　Ｎｏ．１, 2002, ｐ．７７-８３
JPN6012014449; Ｊｏｕｒｎａｌ　ｏｆ　Ｌａｂｅｌｌｅｄ　Ｃｏｍｐｏｕｎｄｓ　＆　Ｒａｄｉｏｐｈａｒｍａｃｅｕｔｉｃａｌｓ ４２（３）, 1999, ｐ．２１５-２２５

Akihiro Otsuka
Fumie Kurosaki

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