General rapid C-[11C]Methylation and C-[18F]Fluoromethylation: Re | 48038

Journal of Neurology & Neurophysiology

ISSN - 2155-9562

General rapid C-[11C]Methylation and C-[18F]Fluoromethylation: Revolutionary advanced method for synthesis of short-lived PET probes

International Conference and Exhibition on Neurology & Therapeutics

May 14-16, 2012 Embassy Suites Las Vegas, USA

Masaaki Suzuki

Scientific Tracks Abstracts: J Neurol Neurophysiol

Abstract :

Positron emission tomography (PET) is a powerful noninvasive method for the investigation of in vivo biochemistry, especially in the human organ. The need for the development of new PET probes has grown with the increase in its use for diagnosis in medicine and for drug development processes in an early stage (microdosing concept). Accordingly, we realized rapid [ 11 C] methylation on various carbon frameworks such as arene, alkyne, alkene, and alkane to establish four kinds of Rapid C-[ 11 C] methylations including heteroaromatics by Pd(0)-mediated reaction of [ 11 C]H 3 I and organotributylstannanes or alkoxyborons. Rapid C-[ 18 F]fluoromethylation were also elaborated by Pd(0)-mediated reactions of [ 18 F]fluoromethyl iodide (or bromide) using an alkoxyorganoboron precursor. Such methylations would realize 11 C and 18 F-labeling of almost any organic compounds, allowing the PD/PK studies by PET in both animals and human to promote ?Evidence-based Medicine?. Actually, methylation on an arene framework was applied to 11 C incorporation into 15R-TIC, a stable prostaglandin analogue, which selectively binds with a novel prostacyclin receptor (IP 2 ) in the central nervous system. 15R-[ 11 C]TIC methyl ester obtained in high yield was used for PET studies (intravenous administration) to visualize IP2 receptor distributed in monkey and human brains in addition to the hepatobiliary transport in rat and human abdomens. The talk also includes the syntheses of Celecoxib metabolite [ 11 C]SC-62807, [methyl- 11 C]]thymidine and its stable analogue 4?-[methyl- 11 C]thiothymidine (biomarker in cancer diagnosis), [ 11 C]all-trans- retinoic acid, 11 C-labeled 2-arylpropionic acids and their esters, [ 11 C]acromelic acid A derivative (inhibitor of neuropathic pain), [ 11 C]H-1152, specific Rho-kinase inhibitor, [ 11 C]dehydropravastation, a probe for transporters in the liver.

Biography :

Assistant Professor, Department of Chemistry, Faculty of Science, Nagoya University (collaborated with Prof. Yoshimasa. Hirata and then with Prof. Ryoji Noyori), 1975-1983 Associate Professor (collaborated with Prof.Ryoji Noyori), Department of Chemistry, Faculty of Science, Nagoya University, 1983-1990 Associate Professor, Chemical Instrument Center, Nagoya University, 1990-1993 Professor, Department of Applied Chemistry, Gifu University, 1993-1998 Professor, Department of Biomolecular Science, Faculty of Engineering, Gifu University,1998-2002 Professor, Regeneration and Advanced Medical Science, Graduate School of Medicine, Gifu University, 2002 ∼ 2008 Emeritus and visiting Professor of Gifu University, 2008 ∼ Deputy Director, RIKEN Center for Molecular Imaging Science, Molecular Imaging Medicinal Chemistry Laboratory, and Team Leader, 2008 ∼