Development of Green and Novel Catalytic Carbon-Carbon Bond Forming Reactions

2015 Fiscal Year Final Research Report

• Project/Area Number: 25410036
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Organic chemistry
• Research Institution: Tokyo Institute of Technology
• Principal Investigator: Aikawa Kohsuke 東京工業大学, 理工学研究科, 助教 (30401532)
• Project Period (FY): 2013-04-01 – 2016-03-31
• Keywords: 有機フッ素化学 / フッ素化 / トリフルオロメチル化 / 触媒的不斉合成 / パラジウム触媒 / ルイス酸 / 含フッ素医薬品 / フルオロアルキル

Outline of Final Research Achievements

The building-block methodology employing readily available fluoroalkyl- containing substances plays a prominent role in catalytic asymmetric synthesis of chiral fluoroalkylated compounds. Thus, chiral alpha-fluoroalkylated tertiary alcohols have received increasingly attention in the field of pharmaceutical science. A number of non-steroidal glucocorticoid receptor modulators bearing the chiral alpha-fluoroalkylated tertiary alcohols were found to possess anti-inflammatory effects of a glucocorticoid but with reduced adverse effects, and hence have been searched as potential therapeutics for various inflammatory diseases, such as asthma, rheumatoid arthritis, and allergic rhinitis. In this research, we have succeeded in the development of practical synthetic methods of valuable and multi-functionalized derivatives of chiral alpha-fluoroalkyl substituted tertiary alcohol and these analogues.

Free Research Field

有機合成化学