Tetrahedron Letters

Regioselective methylation of indazoles using methyl 2, 2, 2-trichloromethylacetimidate

SR Baddam, NU Kumar, AP Reddy, R Bandichhor

Index: Baddam, Sudhakar Reddy; Uday Kumar; Panasa Reddy; Bandichhor, Rakeshwar Tetrahedron Letters, 2013 , vol. 54, # 13 p. 1661 - 1663

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Citation Number: 5

Abstract

Considering therapeutic potential of this class of the molecules, it becomes extremely important to devise an efficient regioselective methylation of substituted 2-methyl-2H-indazoles. Indazoles are found to undergo unselective alkylation under basic conditions to afford corresponding mixture of N-1 and N-2 products, respectively whereas, under mild acidic conditions, regio selective alkylation at N-2 position takes place. N-1 alkylated products are thermodynamically controlled and ...