1445994-07-9Relevant academic research and scientific papers
Diarylation of N- and O-nucleophiles through a metal-free cascade reaction
Bulfield, David,Kervefors, Gabriella,Linde, Erika,Olofsson, Berit,Purkait, Nibadita
, p. 850 - 865 (2022/03/14)
The arylation of heteroatom nucleophiles is a central strategy to reach diarylated compounds that are key building blocks in agrochemicals, materials, and pharmaceuticals. Nucleophilic aromatic substitution is a classical tool for such arylations, and recent developments in hypervalent iodine-mediated arylations allow a wider scope of products. Herein, we combine the benefits of these strategies to enable an efficient and transition-metal-free difunctionalization of N- and O-nucleophiles with two structurally different aryl groups and to provide di- and triarylamines and diaryl ethers in one single step (>100 examples). The core of this strategy is the unique reactivity discovered with specifically designed fluorinated diaryliodonium salts, which unveils novel reaction pathways in hypervalent iodine chemistry. The methodology is suitable for diarylation of aliphatic amines, anilines, ammonia, and even water. It tolerates a wide variety of functional and protecting groups, with the retained iodine substituent easily accessible for derivatization of the products.
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor
McDaniel, Keith F.,Wang, Le,Soltwedel, Todd,Fidanze, Steven D.,Hasvold, Lisa A.,Liu, Dachun,Mantei, Robert A.,Pratt, John K.,Sheppard, George S.,Bui, Mai H.,Faivre, Emily J.,Huang, Xiaoli,Li, Leiming,Lin, Xiaoyu,Wang, Rongqi,Warder, Scott E.,Wilcox, Denise,Albert, Daniel H.,Magoc, Terrance J.,Rajaraman, Ganesh,Park, Chang H.,Hutchins, Charles W.,Shen, Jianwei J.,Edalji, Rohinton P.,Sun, Chaohong C.,Martin, Ruth,Gao, Wenqing,Wong, Shekman,Fang, Guowei,Elmore, Steven W.,Shen, Yu,Kati, Warren M.
supporting information, p. 8369 - 8384 (2017/11/03)
The development of bromodomain and extraterminal domain (BET) bromodomain inhibitors and their examination in clinical studies, particularly in oncology settings, has garnered substantial recent interest. An effort to generate novel BET bromodomain inhibi
BROMODOMAIN INHIBITORS
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Page/Page column 104, (2013/07/19)
Provided are compounds of formula (I), wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
