Tetrahedron

Synthesis of 2-substituted-7-azaindoles from 2-amino-3-picolin

J Parcerisa, M Romero, MD Pujol

文献索引：Parcerisa, Javier; Romero, Manel; Pujol, Maria Dolors Tetrahedron, 2008 , vol. 64, # 3 p. 500 - 507

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被引用次数: 13

摘要

An easy route to the synthesis of 2-substituted-7-azaindole derivatives has been developed. The carbinol intermediate dissolved in DMF undergoes cyclization upon treatment with sodium hydride, trifluoroacetic anhydride, and trifluoroacetic acid at 120° C in a straightforward and one-pot step. An alternative methodology using (CF3SO2) 2O in acetonitrile in basic media followed by the addition of CF3COOH affords the expected 2- ...