460053-59-2Relevant articles and documents
An effective procedure for the preparation of 3-substituted-4- or 6-azaindoles from ortho-methyl nitro pyridines
Zhu, Juliang,Wong, Henry,Zhang, Zhongxing,Yin, Zhiwei,Meanwell, Nicholas A.,Kadow, John F.,Wang, Tao
, p. 5653 - 5656 (2007/10/03)
3-Substituted-4- and 6-azaindoles were prepared from ortho-methyl-nitropyridines in a practically convenient, one-pot process based on the Leimgruber-Batcho reaction. The procedure comprises a sequence of (a) condensation of an ortho-methyl-nitropyridine with N,N-dimethylformamide dimethyl acetal; (b) alkylation or acylation of the enamine intermediate; (c) reduction of the nitro group to an aniline with in situ cyclization and elimination of dimethylamine to generate the 3-substituted azaindole heterocycle.
An effective procedure for the acylation of azaindoles at C-3
Zhang, Zhongxing,Yang, Zhong,Wong, Henry,Zhu, Juliang,Meanwell, Nicholas A.,Kadow, John F.,Wang, Tao
, p. 6226 - 6227 (2007/10/03)
Conditions for attachment of acetyl chloride, benzoyl chloride, and chloromethyl oxalate to the 3-position of 4-, 5-, 6-, or 7-azaindoles were explored. Best results were achieved with an excess of AlCl3 in CH2Cl2 followed