5425-74-1Relevant academic research and scientific papers
[2+2] Photodimerization of Stilbazoles Promoted by Oxalic Acid in Suspension
Nguyen, Thanh Binh,Nguyen, Tuan Minh,Retailleau, Pascal
supporting information, p. 4682 - 4689 (2020/04/15)
In this study, a very simple technique to perform efficiently photodimerization of some vinylpyridines is reported. By irradiating a stirred mixture of several stilbazoles with solid oxalic acid dihydrate dispersed in a nonpolar (i.e., cyclohexane) or moderately polar (benzene, dichloromethane, dioxane) solvent, the corresponding dimeric cyclobutane adducts were obtained in high yields and excellent regio- and stereoselectivities. The strategy could also be applied successfully to oily, waxy, or even insoluble stilbazoles. Moreover, the oxalic acid loading could be lowered to substoichiometric amounts. When further optimizations were needed, our strategy was found to be highly flexible to identify other oligocarboxylic acids as alternative additives to improve, or even overturn, the regioselectivity. Oxalic acid and other oligocarboxylic acids were found to be capable of orienting more than 50 stilbazoles toward photodimerization under these conditions.
A novel D-glucosamine-derived pyridyltriazole@ palladium catalyst for solvent-free Mizoroki-Heck reactions and its application in the synthesis of Axitinib
Shen, Chao,Shen, Hongyun,Yang, Ming,Xia, Chengcai,Zhang, Pengfei
supporting information, p. 225 - 230 (2018/04/16)
A green method for the synthesis of a D-glucosamine-derived triazole@ palladium catalyst is described. The synthesized catalyst containing a 2-pyridyl-1,2,3-triazole ligand was prepared via a click route in high yields and was explored in Heck cross-coupling reactions between different aryl halides and olefins under solventfree conditions. The catalyst can be separated from the reaction mixture and reused at least six times with superior activity. In addition, using this protocol, the marketed drug Axitinib (antitumor) could be synthesized easily.
Lewis-acid-catalyzed benzylic reactions of 2-methylazaarenes with aldehydes
Mao, Dan,Hong, Gang,Wu, Shengying,Liu, Xin,Yu, Jianjun,Wang, Limin
, p. 3009 - 3019 (2014/05/20)
Lewis-acid-catalyzed benzylic reactions of 2-methylazaarenes with aldehydes have been investigated. Series of azaarene derivatives were afforded by this reaction. 2-(Pyridin-2-yl)ethanols with common substituents were formed through the LiNTf2-promoted aldol reaction for the first time. 2-Alkenylpyridines, exclusively in the form of the E isomers, were synthesized in the presence of LiNTf2 cooperated with H2NTf. In the presence of La(Pfb)3 as catalysis, 2-alkenylquinolines were obtained in high yields through the reactions between 2-methylquinolines and aldehydes under air.
Compounds for use as therapeutic agents affecting p53 expression and/or activity
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Page/Page column 45, (2012/10/18)
The present invention relates to compound (I) wherein R1 and R2 independently represent a hydrogen atom, a (C1-C4)alkoxy group, a fluoro(C1-C4)alkoxy group, a hydroxyl group, a benzyloxy group, a di(C1-C4)alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a -NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C1-C4)alkyl group, a CONHR6 group, a -CONR7R8 group, a -SO2NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a -(CH2)nNR7R8 group or a hydroxy(C1-C4)alkyl group; R6 represents a hydrogen atom, a -(CHR9)m(CH2)nNR7R8 group or a (C1-C6)alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use as an agent for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the invention.
Pyridine derivatives
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Page column 14, (2008/06/13)
A compound of formula I wherein X represents an optionally halo-substituted (C2-4)alkynylene group bonded via vicinal unsaturated carbon atoms.
