1060801-42-4Relevant articles and documents
Amination of Aromatic Halides and Exploration of the Reactivity Sequence of Aromatic Halides
Yang, Chu,Zhang, Feng,Deng, Guo-Jun,Gong, Hang
, p. 181 - 190 (2019/01/10)
A base-promoted amination of aromatic halides has been developed using a limited amount of dimethylformamide (DMF) or amine as an amino source. Various aryl halides, including F, Cl, Br, and I, have been successfully aminated in good to excellent yields. Although the amination of aromatic halides with amines or DMF is usually considered as an aromatic nucleophilic substitution (SNAr) process, and the reactivity of an aromatic halide is F > Cl > Br > I, the reactivity of aromatic halides in this system was found to be I > Br a‰ F > Cl. This protocol also showed a good regioselectivity for multihalogenated aromatics. This protocol is valuable for industrial application due to the simplicity of operation, the unrestricted availability of amino sources and aromatic halides, transition metal-free conditions, no requirement for solvent, and scalability.
HETEROARYLSULFONYL-SUBSTITUTED PYRIDINES AND THEIR USE IN THE TREATMENT OF CANCER
-
Page/Page column 46, (2018/09/08)
There is provided compounds of formula I (I) or pharmaceutically-acceptable salts thereof, wherein L, R1, R2, R3 and X have meanings provided in the description, which compounds are useful in the treatment of cancers.