| Budget Amount *help |
¥18,720,000 (Direct Cost: ¥14,400,000、Indirect Cost: ¥4,320,000)
Fiscal Year 2015: ¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2014: ¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2013: ¥10,270,000 (Direct Cost: ¥7,900,000、Indirect Cost: ¥2,370,000)
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| Outline of Final Research Achievements |
Fluorine-containing organic molecules play a pivotal role in the remarkable progress of medicinal, agricultural, and material sciences. Difluoromethylene compounds have been considerable synthetic targets because of their wide utility. Among them, difluoromethylated aromatic compounds (Ar-CF2-R) have received a great deal of attention in the design of bioactive molecules. Previously, we reported the reaction sequence involving cross-coupling and decarboxylation to afford difluoromethyl aromatics (Ar-CF2H). Herein we developed versatile decarboxylative transformations for the synthesis of aromatic compounds bearing functionalized difluoromethyl groups. Upon heating in DMSO or NMP at 170 °C with CuI, potassium 2-aryl-2,2-difluoroacetates underwent decarboxylation to generate aryldifluoromethyl anions (ArCF2-), which reacted with electrophiles to afford a variety of gem-difluoromethylene compounds in moderate to good yields.
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