Journal of Combinatorial Chemistry 2007-01-01

Synthesis of a library of 2-alkyl-3-alkyloxy-2H-indazole-6-carboxamides.

Aaron D Mills, Patrick Maloney, Elsayed Hassanein, Makhluf J Haddadin, Mark J Kurth

Index: J. Comb. Chem. 9(1) , 171-7, (2007)

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Abstract

A library of 200 2-alkyl-3-alkyloxy-2H-indazole-6-carboxamides was synthesized using parallel solution-phase methods. The indazole cyclization reaction was optimized for library production with the best yields resulting from controlled alcohol/water solvent ratios. The key step, a heterocyclization reaction, proceeds by N,N-bond formation and delivers the 2H-indazole scaffold. Automated preparative HPLC was utilized to provide pure compounds on a 10+ mg scale.