Drug Design of Fluorinated Quinolone Carboxylic Acid Related Compounds and the Test of Biological Activities.

点击翻译按钮获取中文摘要

Trifluoroacetimidoyl metals (Li, Zn, Pd, Si) and telluride (1) have been prepared as precursors for the trifluoroacetimidoyl carbanion and the corresponding radicals and have been employed for the syntheses of fluorinated nitrogen heterocycles. Photolysis of the telluride and the iodide leads to homolytic cleavage of the C-Te and C-I bonds to generate the desired trifluoroacetimidoyl radical which undergoes intramolecular cyclization. The reaction provided 3-oxy-2-trifluoromethyl indols (3) , (5) . Meanwhile, palladium catalyzed carboalkoxylation of the trifluoroacetimidoyl iodides and subsequent alkylation and hydrogenation provided various kinds of fluorinated alpha-aminoacids. Optical active trifluoroalanine (2) was synthesized. Lithium-iodine exhange reaction of the iodides generated the acetimidoyl lithium which is stable below -65ﾟC and alkylated. By these newly developed methods, some interesting heterocycles (3) - (6) have been synthesized.