Copper(Ⅰ)-Catalyzed, One-pot Synthesis Of Multisubstituted Indoles

This thesis consists two parts:The first part is a summation. The summation mainly describes the synthesis of indoles nine representative methods, such as Fischer Strategy, Mori Strategy, Hemetsberger Strategy, Buchwald Strategy, Sundberg Strategy, Madelung Strategy, Nenitzescu Strategy, Van leusen Strategy and Kanematsu Strategy. In this review, we have tried to be inclusive, but certainly not comprehensive.The second part introduces our works about synthesis of multisubstituted indole. Reactions of2-iodoanilines with ethyl buta-2,3-dienoate catalyzed by potassium carbonate and CuI in one pot produce the corresponding ethyl2-methyl-lH-indole-3-carboxylate products. The method includes a two-step reaction of Michael addition and Heck coupling. K2CO3is not only a catalyst in Michael addition reaction but also a alkali in the Heck coupling reaction. All products were further characterized by1H NMR,13C NMR, HRMS, FT-IR.