Direct annulation and alkylation of indoles with 2-aminobenzyl alcohols catalyzed by TFA

作者：Robertson Forest J; Kenimer Bradshaw D; Wu Jimmy^*

来源：Tetrahedron, 2011, 67(24): 4327-4332.

DOI：10.1016/j.tet.2011.02.067

• Annulation
• Alkylation
• Indole
• Communesin
• Alcohol

An efficient method for the annulation of indoles with 2-aminobenzyl alcohols, catalyzed by TFA, to furnish 5,6-fused indoline aminals is reported. This method can be extended to the alkylation of indoles at C3. 2-Aminobenzyl alcohols are used directly without recourse to protection of the aniline nitrogen or activation of the alcohol.

• 出版日期2011-6-17