Mild and efficient cyclization reaction of 2-ethynylaniline derivatives to indoles in aqueous medium

作者：Hiroya K^*; Itoh S; Sakamoto T

来源：Tetrahedron, 2005, 61(46): 10958-10964.

DOI：10.1016/j.tet.2005.08.098

• indole
• copper(II) salt
• 2-ethynylaniline
• cyclization reaction

Results of the optimized cyclization reaction of 2-ethynyl aniline derivatives to indoles catalyzed by copper(II) salts are described. The reactions can be carried out in a mixture of H(2)O and MeOH in the presence of 1-ethylpiperidine at room temperature. These conditions can be applied to a bulky substrate, which is difficult to be cyclized efficiently by existing reaction conditions. Furthermore, this reaction condition was applied to a catalyst recycling reaction system.

• 出版日期2005-11-14