460053-59-2Relevant academic research and scientific papers
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.
6-AZAINDOLE COMPOUND
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Page/Page column 78, (2008/06/13)
A compound represented by the formula (I) wherein R1, R2, R3 and R6 are the same or different and each is a hydrogen atom or a substituent; one of R4 and R5 is a hydrogen atom and the other is a group represented by the formula: -C(=X)-R7 wherein X is N-O-R8 or N-NH-R9 wherein R8 and R9 are the same or different and each is a hydrogen atom or a group bonded via a carbon atom; and R7 is a hydrogen atom or a substituent, and the like and a salt thereof have a superior IκB kinase inhibitory activity, and useful as pharmaceutical agents such as agents for preventing or treating diabetes and the like.
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
