1689-02-7Relevant articles and documents
NEW BRAF INHIBITORS AS PARADOX BREAKERS
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Page/Page column 43-44, (2021/06/22)
The invention provides a novel compound having the general formula (I) (I) wherein R1-R3 and X are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
S(vi) in three-component sulfonamide synthesis: Use of sulfuric chloride as a linchpin in palladium-catalyzed Suzuki-Miyaura coupling
Wang, Xuefeng,Yang, Min,Ye, Shengqing,Kuang, Yunyan,Wu, Jie
, p. 6437 - 6441 (2021/05/19)
Sulfuric chloride is used as the source of the -SO2- group in a palladium-catalyzed three-component synthesis of sulfonamides. Suzuki-Miyaura coupling between the in situ generated sulfamoyl chlorides and boronic acids gives rise to diverse sulfonamides in moderate to high yields with excellent reaction selectivity. Although this transformation is not workable for primary amines or anilines, the results show high functional group tolerance. With the solving of the desulfonylation problem and utilization of cheap and easily accessible sulfuric chloride as the source of sulfur dioxide, redox-neutral three-component synthesis of sulfonamides is first achieved. This journal is
Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides
Russell, Stephanie,Rahmani, Rapha?l,Jones, Amy J.,Newson, Harriet L.,Neilde, Kevin,Cotillo, Ignacio,Rahmani Khajouei, Marzieh,Ferrins, Lori,Qureishi, Sana,Nguyen, Nghi,Martinez-Martinez, Maria S.,Weaver, Donald F.,Kaiser, Marcel,Riley, Jennifer,Thomas, John,De Rycker, Manu,Read, Kevin D.,Flematti, Gavin R.,Ryan, Eileen,Tanghe, Scott,Rodriguez, Ana,Charman, Susan A.,Kessler, Albane,Avery, Vicky M.,Baell, Jonathan B.,Piggott, Matthew J.
, p. 9686 - 9720 (2016/11/19)
The parasitic trypanosomes Trypanosoma brucei and T. cruzi are responsible for significant human suffering in the form of human African trypanosomiasis (HAT) and Chagas disease. Drugs currently available to treat these neglected diseases leave much to be