853793-24-5Relevant academic research and scientific papers
A Direct Approach to Decoration of Bioactive Compounds via C-H Amination Reaction
Ju, Guodong,Yuan, Chunchen,Wang, Dongjie,Zhang, Jingyu,Zhao, Yingsheng
supporting information, p. 9852 - 9855 (2019/12/24)
The development of new methods to achieve the direct synthesis of bioactive organic molecules is always an important topic in organic synthesis. We hereby demonstrate that N-methoxyamide is an excellent amino source in the iridium-catalyzed intermolecular C-H amination reaction. The linkage of two bioactive organic molecules can be well achieved with this new protocol. More than 20 examples of decorated bioactive compounds were reported, which can facilitate the discovery of new bioactive molecules.
An efficient route to 3-trifluoromethylpyrazole via cyclization/1,5-H shift and its applications in the synthesis of bioactive compounds
Wang, Yongdong,Han, Jing,Chen, Jie,Cao, Weiguo
, p. 8256 - 8262 (2015/10/05)
A methodology for regioselective synthesis of 3-trifluoromethylpyrazole from the reaction of trifluoromethyl alkenone and tosylhydrazone has been developed. The reaction was proposed to proceed through a tandem cyclization and 1,5-H shift reaction, which can be applied to the synthesis of bioactive compounds like Celecoxib, Mavacoxib, and SC-560.
Silver-mediated cycloaddition of alkynes with CF3CHN 2: Highly regioselective synthesis of 3-trifluoromethylpyrazoles
Li, Feng,Nie, Jing,Sun, Long,Zheng, Yan,Ma, Jun-An
, p. 6255 - 6258 (2013/07/05)
Silver screen: The title reaction provides a convenient and efficient method for the construction of 5-substituted 3-trifluoromethylpyrazoles under mild reaction conditions. By using this protocol, the marketed drug Celecoxib (antiarthritic) could be easily synthesized (see scheme; DMF=N,N- dimethylformamide). Copyright
A novel three-step synthesis of Celecoxib via palladium-catalyzed direct arylation
Gaulier, Steven M.,McKay, Reuben,Swain, Nigel A.
, p. 6000 - 6002 (2011/11/28)
A novel three linear step synthesis of Celecoxib was achieved in 33% overall yield via a key regioselective direct C-H arylation reaction between a 1,3-disubstituted pyrazole and an aryl bromide.
