National Institute of Radiological Sciences

Taisho Pharmaceutical Co., Ltd.

Nihon Nohyaku Co., Ltd.

Kazutoshi Suzuki

Ming-Rong Zhang

Atsuro Nakazato

Tetsuya Suhara

Makoto Goto

Katsushi Kumata

A phenyl tin compound is synthesized by using a derivative having various functional groups and a bromo- or iodo-benzene ring as a labeling material of a radioactive ligand. On the other hand, a novel hydroxytosyl iodobenzene compound having an electron-donating group is obtained by oxidizing iodobenzene having one or more electron-donating groups and reacting it with tosylic acid. Then, a diphenyliodonium salt which is a labeling precursor is synthesized by reacting the resulting compound with various phenyl tin compounds. Finally, aF-labeled ligand having various functional groups and a [F] fluorobenzene ring is synthesized by reacting the resulting diphenyliodonium salt with [F]F.

[object Object]

A phenyloxyaniline derivative useful as a ligand for peripheral benzodiazepine receptor having a strong affinity and a high selectivity, which is represented by formula (1):wherein Xand Xare same or different and each is hydrogen atom or halogen atom; Rand Rare same or different and each is hydrogen atom, an alkyl group having 1 to 10 carbon(s) or a halogen-substituted alkyl group having 1 to 10 carbon(s); and Ris a halogen-substituted alkyl group having 1 to 5 carbon(s), or a radioisotope thereof.

Phenyloxyaniline derivatives

Growing community of inventors

Chiba, Japan

Kazutoshi Suzuki