Article

Synthesis of 1,6-dihydropyrrolo[2,3-g]indazoles using Larock indole annulation

Tetrahedron 01/2011; 67(38):7330-7335. DOI:10.1016/j.tet.2011.07.029 ISBN: 0040-4020

ABSTRACT The synthesis of 1,6-dihydropyrrolo[2,3-g]indazole derivatives is described. The indolic ring system is constructed via a Larock palladium-catalyzed annulation using terminal and internal alkynes. Additionally, when using internal alkynes for this reaction, we found that a directing effect on regioselectivity was mediated by the ester group of alkyl 3-substituted propiolate derivatives.

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