Research Direction in English


 1. 生物活性化合物の合成
 2. 酵素触媒不斉合成法の開発
 3. ベンザインの反応制御と合成化学的応用
 4. 創薬や医療に資する新規機能性分子の精密有機合成
 具体的には、特異な化学構造と顕著な生物活性を有するallocolchicine, aloin, bryostatin, viridinなどの全合成研究とそれらの誘導体創製を行っている。そのために、「典型元素」、「遷移金属」、「酵素」などの特性を活かし、また潜在能力を引き出し、更にこれらを融合した新しい合成手法を開発している。例えば、「加水分解酵素リパーゼと固定化金属触媒を組み合わせた不斉合成法」、「芳香族化合物への位置選択的フッ素導入法」、「高反応活性なベンザインの反応性制御による多置換縮環芳香族化合物の合成法」、「マクロライド類の網羅的立体制御合成法」などを開発している。すでに一部の成果を国際的な専門誌に発表し、また、特許を取得し、世界的に注目され高い評価を得ている。さらに、我々が合成した新規な医薬品候補化合物や独自の触媒や合成法を、創薬シーズ分子の創出、医農薬の効率的製造、革新的医療へと繋げるべく、他領域の研究グループとの共同研究を積極的に行っている。

Research Direction

 Most of active substances of medicines are functional organic molecules, both naturally occurring and man-made, and complex biological processes in living organisms are accurately controlled by chemical interplay of organic molecules at the molecular level. In this sense, organic chemistry has been playing critical roles for drug discovery. Nowadays, the development of environmentally benign methods for producing medicines is another urgent challenge. As a means to accommodate these requests, our research group has been engaged in (1) the syntheses of biologically important natural products and their derivatives as well as artificial molecules which are expected to become drug candidates and (2) the creation of new synthetic methods, strategies and catalysts. Some of the noteworthy projects and results are as follows:
 We have been studying total syntheses of bioactive natural products, such as allocolchicine, aloin, viridin and their derivatives. The purpose of our total syntheses involves not only creating a process for retrieving a large supply of target compounds but also designing new functional molecules that would serve as potent leads for future drug discovery. For this purpose, the known synthetic methods are not always satisfactory, and therefore, we also have focused our efforts on devising new methods to find solutions by best employing characteristic features of typical elements, transition metals, enzymes, etc. A typical example is given by the lipase/oxovanadium combo-catalyzed dynamic kinetic resolution that quantitatively converts racemic alcohols into optically pure molecules. Effective utilization of very reactive species, such as benzynes, as key synthetic intermediates, is our other big projects to construct complex molecules in single steps. We have also developed methods for regioselective deoxyfluorination of benzenes to effectively produce fluorinated molecules which are of particular interest as drug candidates.
 Interdisciplinary research is also currently underway through cooperation with other research groups, pursuing pharmacological evaluations of the synthesized compounds as well as gaining vital clue to understanding of their biological functions.