1001014-61-4Relevant academic research and scientific papers
Rhodium-catalyzed regioselective C(sp2)–H bond activation reactions of N-(hetero)aryl-7-azaindoles and cross-coupling with α-carbonyl sulfoxonium ylides
Tian, Yan,Kong, Xian-Qiang,Niu, Jie,Huang, Yi-Bo,Wu, Zhao-Hua,Xu, Bo
, (2020)
We described a protocol for rhodium-catalyzed C(sp2)–H bond activation reactions of N-(hetero)aryl-7-azaindoles and cross-coupling with α-carbonyl sulfoxonium ylides. In the C–H activation reaction, the 7-azaindole moiety acts as a directing gr
Mechanochemical Solvent-Free Catalytic C?H Methylation
Ni, Shengjun,Hribersek, Matic,Baddigam, Swarna K.,Ingner, Fredric J. L.,Orthaber, Andreas,Gates, Paul J.,Pilarski, Lukasz T.
supporting information, p. 6660 - 6666 (2020/12/18)
The mechanochemical, solvent-free, highly regioselective, rhodium-catalyzed C?H methylation of (hetero)arenes is reported. The reaction shows excellent functional-group compatibility and is demonstrated to work for the late-stage C?H methylation of biologically active compounds. The method requires no external heating and benefits from considerably shorter reaction times than previous solution-based C?H methylation protocols. Additionally, the mechanochemical approach is shown to enable the efficient synthesis of organometallic complexes that are difficult to generate conventionally.
Ruthenium-Catalyzed Direct and Selective C-H Cyanation of N-(Hetero)aryl-7-azaindoles
Mishra, Aniket,Vats, Tripta Kumari,Deb, Indubhusan
, p. 6525 - 6534 (2016/08/16)
An efficient, highly regioselective, and scalable ruthenium-catalyzed o-aryl C-H mono-cyanation of N-aryl-7-azaindoles to form N-(2-cyanoaryl)-7-azaindoles has been developed through N-directed ortho C-H activation using N-cyano-N-phenyl-p-toluenesulfonam
Rhodium-catalyzed regioselective C-H chlorination of 7-azaindoles using 1,2-dichloroethane
Qian, Guangyin,Hong, Xiaohu,Liu, Bingxin,Mao, Hong,Xu, Bin
supporting information, p. 5294 - 5297 (2015/01/09)
An unexpected rhodium-catalyzed regioselective C-H chlorination of 7-azaindoles was developed using 1,2-dichloroethane (DCE) as a chlorinating agent and 7-azaindole as the directing group. This protocol provides an efficient access to ortho-chlorinated azaindoles with operational simplicity, good functional group tolerance, and a wide substrate scope. (Chemical Equation Presented).
SELECTIVE AZOLE PDE10A INHIBITOR COMPOUNDS
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Page/Page column 172, (2010/11/29)
The invention pertains to heteroaromatic compounds of the formula I, as defined herein, that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.
