Riken Corporation

Hamamatsu-photonics K.k.

Ge Healthcare Limited

Gifu University

Hisashi Doi

Masaaki Suzuki

Yasuyoshi Watanabe

Miki Goto

Ryoji Noyori

Bengt Langstrom

Satoshi Obika

Takamitsu Hosoya

Takeshi Imanishi

Farhad Karimi

Hideo Tsukada

Hiroko Koyama

Misato Takashima

Miho Shukuri

Hirotaka Onoe

Julien Barletta

Takeshi Kuboyama

Kayo Takahashi

Provided is a method whereby a heteroaromatic ring aryl can be very rapidly methylated at a high yield. In an N-alkyl-2-pyrrolidinone, a heteroaromatic ring aryltrialkylstannan is cross-coupled with methyl iodide in the presence of a palladium complex, a phosphine ligand, a cuprous halide, a carbonic acid salt and/or an alkali metal fluoride to thereby rapidly methylate the heteroaromatic ring aryl. (Formula shows a case wherein the heteroaromatic ring aryl is a pyridyl group.) 

Method for rapidly methylating heteroaromatic arene and method for producing tracer for use in PET

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

Methods and reagents for transition metal-promoted carbonylation via isocyanate using carbon-isotope labeled carbon monoxide are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.

Methods for carbon isotope labeling synthesis by transition metal-promoted carbonylation via isocyanate using azides and carbon-isotope monoxide

The present invention provides anF-labeled azide compound usable in the Huisgen reaction which enablesF-labeling although only a small quantity of alkyne compound is available as a counterpart substrate, more specifically theF-labeled azide compound enabling the PET to be applied to peptides or oligonucleotides and enabling theF-labeling of any sites of oligonucleotide other than the 5' end or 3&#x2032; end thereof, a reagent forF-labeling, and a method forF-labeling of an alkyne compound using the same.

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A method of rapid methylation of an aromatic compound or an alkenyl compound, which is capable of obtaining an aromatic compound or an alkenyl compound labeled with a methyl group or a fluoromethyl group under a mild condition rapidly in high yield using an organic boron compound whose toxicity is not so high as a substrate. A kit for preparing a PET tracer and a method of producing a PET tracer can be practiced using the rapid methylation method. In an aprotic polar solvent, methyl iodide or X&#x2014;CH2F (wherein X is a functional group which can be easily released as an anion), and an organic boron compound in which an aromatic ring or an alkenyl group is attached to boron are subjected to cross-coupling in the presence of a palladium(0) complex, a phosphine ligand, and a base.

Method of rapid methylation, kit for preparing PET tracer and method of producing PET tracer

Growing community of inventors

Kobe, Japan

Hisashi Doi