Our team is developing the general synthetic methodology of short-lived PET molecular probes for promotion of PET molecular imaging science. With the objective of applying the potentials of organic chemistry to life science, we seek to realize the new synthetic methodology of PET molecular probes by using organometallic catalysts such as Pd, Rh, and Cu etc. As one of our main projects, we are striving toward introducing 11C into carbon frameworks of bioactive organic compounds by developing Pd0-mediated rapid C-[11C]methylations. These labeling methods provides groundbreaking synthesis for introducing the [11C]methyl group as the minimum carbon substituent into a carbon framework in the very short time of 5 minutes (Fig.1). We are currently expanding and evolving these rapid methylations from introduction of [11C]methyl group to [18F]fluoromethyl group, and furthermore developing the stoichiometry-focused 18F-labeling of oligodeoxynucleotides and peptides by the application of Click chemistry (Fig.2).

In the field of PET radiolabeling, the performance of the remote-controlled PET probe synthesizer is of key importance for realizing high quality and high yield in the synthesis of PET molecular probes. In this regard, we are also engaged in developing original PET probe synthesizers from the perspectives of not only safety and quick operation emphasized in labeling chemistry but also introducing advantages of experimental techniques ordinarily-used in organic chemistry. Thus, we seek to realize high quality RIKEN original molecular probes and establish the probe library through developing the new labeling methodology from the perspective of synthetically ideals and efficiencies based on organic chemistry (Fig.3).                                                                                                                                 

In addition, our team is responsible for production of PET drugs for human PET study in three institutions including Osaka City University Hospital.