Nihon Medi-Physics Company, Limited

Toshiyuki Shinmura

Akio Hayashi

Masahito Toyama

Fumie Kurosaki

Osamu Ito

Arinori Harano

Emi Kaneko

Daisaku Nakamura

Soichi Nakamura

Shinji Tokunaga

Soichi Takasaki

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 [F]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; Ris an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by &#x2014;OR; Ris 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 Ris a protective group.

Precursor compound of radioactive halogen-labeled organic compound

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 [F]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; Ris an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by &#x2014;OR; Ris 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 Ris a protective group.

A composition including a radioactive fluorine-labeled amino acid compound is provided, which can be prevented from radiolysis. Disclosed is a composition which includes a solution containing a radioactive fluorine-labeled amino acid compound as an effective ingredient, in which the pH value of the solution is kept at 2.0-5.9, more preferably 2.0-4.9 in order to inhibit radiolysis. Also, it is possible to further inhibit radiolysis by adding thereto a pharmaceutical additive capable of inhibiting radiolysis, such as a sugar, a sugar alcohol and a sugar lactone, while the pH is kept at 2.0-5.9.

Radioactive diagnostic imaging agent

Unnatural amino acid radiolabeling precursor

A process is provided for producing [F]FACBC, which can reduce the production amount of impurities. Disclosed is a process for producing a radioactive fluorine-labeled organic compound, including a deesterification step of retaining, in a reverse-phase column, a compound represented by Formula (1): wherein Ris a linear or branched C-C-alkyl chain or an aromatic substituent, and Ris a protecting group; wherein X is sodium or potassium; and 

Process for production of radioactive fluorine-labeled organic compound

Growing community of inventors

Chiba, Japan

Toshiyuki Shinmura