Tetrahedron

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

K Hiroya, S Itoh, T Sakamoto

Index: Hiroya, Kou; Itoh, Shin; Sakamoto, Takao Tetrahedron, 2005 , vol. 61, # 46 p. 10958 - 10964

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Citation Number: 85

Abstract

Results of the optimized cyclization reaction of 2-ethynylaniline derivatives to indoles catalyzed by copper (II) salts are described. The reactions can be carried out in a mixture of H2O 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 ...