153394-55-9Relevant academic research and scientific papers
Palladium-catalyzed direct addition of arylboronic acids to 2-aminobenzonitrile derivatives: Synthesis, biological evaluation and in silico analysis of 2-aminobenzophenones, 7-benzoyl-2-oxoindolines, and 7-benzoylindoles
Chen, Jiuxi,Ye, Leping,Su, Weike
supporting information, p. 8204 - 8211 (2015/01/08)
A palladium-catalyzed direct addition of arylboronic acids to unprotected 2-aminobenzonitriles has been developed, leading to a wide range of 2-aminobenzophenones with moderate to excellent yields. The transformation has broad scope and high functional group tolerance. Moreover, 2-oxoindoline-7-carbonitrile and indole-7-carbonitrile were applicable to this process for the construction of 7-benzoyl-2-oxoindolines and 7-benzoylindoles, respectively. Among the compounds examined, compound 4e possessed the most potent anticancer activity against H446 and HGC-27 in vitro, with IC50 values of 0.02 μmol L-1 and 0.09 μmol L-1, respectively, while compound 4a showed the best potent anticancer activity against SGC-7901 with an IC50 value of 0.01 μmol L-1. Furthermore, we also performed in silico molecular docking calculations to investigate the interaction mode and binding affinity between the examined compounds and their tubulin target. This journal is
Process development of a disease-modifying antirheumatic drug, TAK-603, based on optimization of Friedel-Crafts reaction and selective substitution of a triazole ring
Mizuno, Masahiro,Inagaki, Atsushi,Yamashita, Makoto,Soma, Norie,Maeda, Yoshiharu,Nakatani, Hiroshi
, p. 4065 - 4070 (2007/10/03)
A practical method for the preparation of TAK-603, an antirheumatic drug, has been developed. As a result of optimizing the Friedel-Crafts reaction in the presence of SnCl4/POCl3, 2-aminobenzophenone skeleton, the key intermediate of
Process for the preparation of 2-amino-4,5,3',4'-tetramethoxybenzophenone
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, (2008/06/13)
2-Amino-4,5,3',4'-tetramethoxybenzophenone of the formula: is prepared by mononitration of 3,3',4,4'-tetramethyoxybenzophenone using nitric acid in the presence of acetic acid, and subsequent reduction of the nitro group. The compound is an intermediate i
