56291-51-1Relevant articles and documents
C2-Selective Branched Alkylation of Benzimidazoles by Rhodium(I)-Catalyzed C-H Activation
Tran, Ga?l,Confair, Danielle,Hesp, Kevin D.,Mascitti, Vincent,Ellman, Jonathan A.
, p. 9243 - 9252 (2017/09/11)
Herein, we report a Rh(I)/bisphosphine/K3PO4 catalytic system allowing for the first time the selective branched C-H alkylation of benzimidazoles with Michael acceptors. Branched alkylation with N,N-dimethyl acrylamide was successfully applied to the alkylation of a broad range of benzimidazoles incorporating a variety of N-substituents and with both electron-rich and -poor functionality displayed at different sites of the arene. Moreover, the introduction of a quaternary carbon was achieved by alkylation with ethyl methacrylate. The method was also shown to be applicable to the C2-selective branched alkylation of azabenzimidazoles.
Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase
Gritzalis, Dimitrios,Park, Jaeok,Chiu, Wei,Cho, Hyungjun,Lin, Yih-Shyan,De Schutter, Joris W.,Lacbay, Cyrus M.,Zielinski, Michal,Berghuis, Albert M.,Tsantrizos, Youla S.
supporting information, p. 1117 - 1123 (2015/02/19)
In order to explore the interactions of bisphosphonate ligands with the active site and an allosteric pocket of the human farnesyl pyrophosphate synthase (hFPPS), substituted indole and azabenzimidazole bisphosphonates were designed as chameleon ligands. NMR and crystallographic studies revealed that these compounds can occupy both sub-pockets of the active site cavity, as well as the allosteric pocket of hFPPS in the presence of the enzyme's Mg2+ ion cofactor. These results are consistent with the previously proposed hypothesis that the allosteric pocket of hFPPS, located near the active site, plays a feed-back regulatory role for this enzyme.
Efficient synthesis of substituted imidazo[4,5-b] pyridine
Xing, Yuan-Yuan,Liu, Chuanxiang,Wu, Fanhong
, p. 327 - 330 (2014/01/06)
An efficient approach to the synthesis of 1-methylimidazo[4,5-b]pyridine derivatives 5-10 of biological interest has been developed. The key intermediate product 4 is obtained by cyclization of 2-amino-3-methylaminopyridine (3) with phenylacetic acid.