5751-51-9Relevant articles and documents
Ruthenium(II)-Catalyzed C-H Activation of Chromones with Maleimides to Synthesize Succinimide/Maleimide-Containing Chromones
Zhou, Yan,Liang, Hong,Sheng, Yaoguang,Wang, Shaoli,Gao, Yi,Zhan, Lingling,Zheng, Zhilong,Yang, Mengjie,Liang, Guang,Zhou, Jianmin,Deng, Jun,Song, Zengqiang
, p. 9230 - 9243 (2020)
An efficient route for the coupling of maleimides with chromones at the C5-position has been developed under Ru(II) catalysis. It could provide 1,4-addition products and oxidative Heck-type products by switching additives. Benzoic acid led to the formation of 1,4-addition products under solvent-free conditions, and silver acetate was promoted to the generation of oxidative Heck-type products. Various maleimides and chromones were suitable for this transformation, affording the desired products with good to excellent yields in a short reaction time. To understand the mechanism of this reaction, deuteration studies and control experiments have been performed.
Substituent-Oriented Synthesis of Substituted Pyrazoles/Chromeno[3,2- c]pyrazoles via Sequential Reactions of Chromones/3-Chlorochromones and Tosylhydrazones
Dai, Tianzi,Li, Qunyi,Zhang, Xiaofei,Yang, Chunhao
, p. 5913 - 5921 (2019/05/10)
A facile and efficient synthetic strategy for the chemoselective synthesis of monocyclic/tricyclic-fused pyrazoles was developed, and it was oriented by different 3-position substituents (H or Cl) on the chromones. The reaction proceeded in a one-pot sequential way with a broad substrate scope and moderate to excellent yields.
Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis
Wang, Xueqing,Liu, Bo,Searle, Xenia,Yeung, Clinton,Bogdan, Andrew,Greszler, Stephen,Singh, Ashvani,Fan, Yihong,Swensen, Andrew M,Vortherms, Timothy,Balut, Corina,Jia, Ying,Desino, Kelly,Gao, Wenqing,Yong, Hong,Tse, Chris,Kym, Philip
supporting information, p. 1436 - 1449 (2018/03/05)
Cystic fibrosis (CF) is a multiorgan disease of the lungs, sinuses, pancreas, and gastrointestinal tract that is caused by a dysfunction or deficiency of the cystic fibrosis transmembrane conductance regulator (CFTR) protein, an epithelial anion channel that regulates salt and water balance in the tissues in which it is expressed. To effectively treat the most prevalent patient population (F508del mutation), two biomolecular modulators are required: correctors to increase CFTR levels at the cell surface, and potentiators to allow the effective opening of the CFTR channel. Despite approved potentiator and potentiator/corrector combination therapies, there remains a high need to develop more potent and efficacious correctors. Herein, we disclose the discovery of a highly potent series of CFTR correctors and the structure-activity relationship (SAR) studies that guided the discovery of ABBV/GLPG-2222 (22), which is currently in clinical trials in patients harboring the F508del CFTR mutation on at least one allele.