Synthesis of an Ethyl 6-Amino-3,5-difluorosalicylate Derivative by Sequential Regioselective Directed ortho-Metalation; A Practical Synthesis of4',5-Diamino-3',6,8-trifluoroflavone, A Potent Antitumor Agent

All articles of this category The multigram scale synthesis of 4',5-diamino-3',6,8-trifluoroflavone, a potent antitumor agent, is described in which regioselective introduction of a carbonyl group into the ortho -position to the amide group of 2-[2,4-difluoro-5-(pivaloylamino)phenoxy]tetrahydropyran is achieved by using sequential direct ortho -metalations as the key step. directed ortho -metalation - Stille coupling - flavone