Tetrahedron letters

Synthesis of functionalized 7-azaindoles via directed ortho-metalations

A L'Heureux, C Thibault, R Ruel

Index: L'Heureux, Alexandre; Thibault, Carl; Ruel, Rejean Tetrahedron Letters, 2004 , vol. 45, # 11 p. 2317 - 2319

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Citation Number: 24

Abstract

7-Azaindole derivatives may be considered as useful indole bioisosteres in medicinal chemistry and functionalization at C-2 and C-3 of the 7-azaindole ring system is well described in the scientific literature. Substitution of the pyrrole ring has been effected either directly on the 7-azaindole core or, alternatively, by cyclization of a requisite pyridine precursor. 1 On the other hand, the limited number of examples of 4-, 5-, and 6-substituted 7-azaindoles reported thus far ...