ジカチオン性パラジウム錯体を用いたフルオロアルキル化合物の触媒的不斉合成

抄録

By virtue of the unique properties of fluorine atom, fluorinated organic compounds often affect pharmaceutical and agrochemical industry. Over the past decades, a variety of methodology for incorporating fluoroalkyl groups, especially trifluoromethyl group, have been developed. On the other hand, the building-block methodology employing readily available fluoroalkyl-containing substances plays a prominent role in catalytic asymmetric synthesis of chiral fluoroalkylated compounds. Thus, chiral α-fluoroalkylated tertiary alcohols have received increasingly attention in the field of pharmaceutical science. A number of non-steroidal glucocorticoid receptor modulators bearing the chiral α-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 paper, we describe the development of practical synthetic methods of valuable and multi-functionalized derivatives of chiral α-fluoroalkyl substituted tertiary alcohol and these analogues.