HOME > Laboratories > Molecular Imaging Labeling Chemistry Laboratory> Research Content

To accelerate and advance the drug discovery process and shed light on vital functions, our laboratory is, in cooperation with the Molecular Imaging Medicinal Chemistry Laboratory, working to develop general synthetic methodologies for short-lived PET probes, which will be fundamental for promoting PET research. In particular, our research is focused on developing PET probe syntheses for drug candidates and novel chemical labeling reactions with the aim of broadening the spectrum of potential applications of organic chemistry in life science research. Furthermore, we are striving toward creating a RIKEN original, high-quality molecular probe(s) that can also be applied to human clinical studies by developing organometallic approaches to radiolabeling and establishing efficient PET probe synthesizers.

As one of our main projects we are striving toward introducing ¹¹C into carbon frameworks of bioactive organic compounds by developing rapid C-[¹¹C]methylation reactions based on carbon-carbon bond formation, focusing on the methyl group as the minimum carbon substituent. We have already succeeded in developing several cross-coupling reactions between organotin or organoboron compounds and [¹¹C]methyl iodide in the presence of palladium catalysts. These reactions are attracting worldwide attention as groundbreaking synthesis for introducing the [¹¹C]methyl group into a carbon framework in the very short time of 5 minutes. We are also conducting the following three projects to further promote PET chemistry:
(1) Development of PET-probe syntheses for drug candidates and novel labeling reactions
(2) Development of remote-controlled synthesizers and efficient synthetic procedures for radiolabeling by organometallic chemistry, and
(3) Establishment of general methodologies for high-quality synthesis of PET probes applicable to human clinical studies.