医薬分野への応用を指向した新しいトリフルオロメチル化合物の合成法の開発

抄録

New reactions developed for the synthesis of medicinally useful trifluoromethyl compounds are discussed. First, the trifluoromethylation of aromatic halogen compounds with CF₃I and Cu powder is presented. This method is applicable to a wide range of aromatic halides, while aliphatic halides cannot be converted to trifluoromethyl compounds. This difficulty was removed by two-step procedure. CF₃I and Cu powder were shaken in a stainless steel tube, and the excess of Cu powder was removed by filtration. The solution of [CF₃-Cu] was treated with halogen compounds to give trifluoromethyl compounds. Next, the Friedel-Crafts reaction of trifluoropropene was presented, which gave trifluoropropyl compounds. It was very difficult to obtain these products by other routes. Attempted application of the trifluoropropyl compounds are included. Finally, some reactions useful for the synthesis of special types of trifluoromethyl compounds were summarized, where photoreaction, 1, 3-dipolar reaction, and ene reaction of trifluoromethyl compounds are included.