Riken Corporation

Miki Goto

Masaaki Suzuki

Hisashi Doi

Yasuyoshi Watanabe

Misato Takashima

Miho Shukuri

Hirotaka Onoe

Provided are: a method for rapid fluoromethylation, by which a fluoromethyl group can be easily bonded to an aromatic-ring carbon of an aromatic compound with little generation of by-products; and a process for preparation of a PET tracer using the same. The method is characterized by cross-coupling an organoboron compound in which an aromatic ring is bonded to a boron atom with FCXBr (wherein X is ordinary hydrogen or heavy hydrogen) in a solvent obtained by adding water to an aprotic polar solvent, in the presence of a palladium complex, a phosphine ligand, and a base.

Method for rapid fluoromethylation and method for preparation of PET tracer using the same

Disclosed are: labeled NSAIDs compounds which can be produced within a short time, can be used suitably for a PET method, and enable the imaging of cyclooxygenase-2; and a process for producing the labeled NSAIDs compounds. Specifically disclosed are isotope-labeled 2-arylpropionic acid compounds, each of which is a compound represented by general formula (1) (wherein Ar represents an aryl group which may have a substituent; Rrepresents anyone selected fromCH, CHF and CFF; and Rrepresents a hydrogen atom, or an alkyl group which may have a branch, wherein a compound wherein Ar is a benzene ring, RisCH, and Ris a hydrogen atom is excluded), or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof.

Isotope labeled 2-arylpropionic acid compounds and process for production of same, and molecular probe for positron emission tomography and method for imaging of cyclooxygenase and the like using same

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Kobe, Japan

Miki Goto