13294-40-1Relevant academic research and scientific papers
Avisible-light-promoted metal-free strategy towards arylphosphonates: Organic-dye-catalyzed phosphorylation of arylhydrazines with trialkylphosphites
Li, Rui,Chen, Xiaolan,Wei, Shengkai,Sun, Kai,Fan, Lulu,Liu, Yan,Qu, Lingbo,Zhao, Yufen,Yu, Bing
supporting information, p. 4807 - 4813 (2018/12/11)
A visible-light-induced metal-free catalytic system was developed for the synthesis of arylphosphonates starting from arylhydrazines and trialkylphosphites. By using the inexpensive eosin B as catalyst, sub-stoichiometric amounts of DABCO, and ambient air as oxidant, diverse arylphosphonates were obtained under visible-light irradiation. Notably, this catalytic system is suitable for gram-scale reaction by utilizing sunlight as an illumination source.
Discovery of benzophosphadiazine drug candidate IDX375: A novel hepatitis C allosteric NS5B RdRp inhibitor
Paparin, Jean-Laurent,Amador, Agnès,Badaroux, Eric,Bot, Stéphanie,Caillet, Catherine,Convard, Thierry,Da Costa, Daniel,Dukhan, David,Griffe, Ludovic,Griffon, Jean-Fran?ois,LaColla, Massimiliano,Leroy, Frédéric,Liuzzi, Michel,Giulia Loi, Anna,McCarville, Joe,Mascia, Valeria,Milhau, Julien,Onidi, Loredana,Pierra, Claire,Rahali, Rachid,Rosinosky, Elodie,Sais, Efisio,Seifer, Maria,Surleraux, Dominique,Standring, David,Dousson, Cyril B.
, p. 2634 - 2640 (2017/05/10)
Hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) plays a central role in virus replication. NS5B has no functional equivalent in mammalian cells, and as a consequence is an attractive target for selective inhibition. This paper describes the discovery of a novel family of HCV NS5B non-nucleoside inhibitors inspired by the bioisosterism between sulfonamide and phosphonamide. Systematic structural optimization in this new series led to the identification of IDX375, a potent non-nucleoside inhibitor that is selective for genotypes 1a and 1b. The structure and binding domain of IDX375 were confirmed by X-ray co-crystalisation study.
Silver-catalyzed highly regioselective phosphonation of arenes bearing electron-withdrawing groups
Mao, Xuerong,Ma, Xiao,Zhang, Shuwei,Hu, Hongwen,Zhu, Chengjian,Cheng, Yixiang
, p. 4245 - 4248 (2013/07/26)
A highly efficient, AgI/K2S2O 8-mediated regioselective phosphonation reaction has been developed by using electron-deficient directing groups. These phosphonation reactions were performed with N,N-dialkylbenzamides, N,N-dialkylbenzenesulfonamides, and nitrobenzene. This method has a broad substrate scope and offers facile construction of C-P bonds. Copyright
AMIDES AS SPHINGOMYELINE INHIBITORS
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Page/Page column 62, (2008/06/13)
The present invention, relates to compounds of formula (I), wherein A is hydrogen or (C1-4)alkyl, R1 is a group Y-R2, Y is not present or is (C1-4)alkylene, which alkylene optionally is substituted, e.g. one or
Synthesis and antibacterial activity of new aryl / alkyl phosphonates via Michaelis-Arbuzov rearrangement
Syam Prasad, Gandavaram,Manjunath, Manubolu,Kishore Kumar Reddy, Kachi Reddy,Sarathi Reddy, Obulam Vijaya,Suresh Reddy, Cirandur
, p. 128 - 135 (2015/01/08)
Synthesis of new aryl / alkyl phosphonates 3a-j has been accomplished via a Michaelis- Arbuzov-type rearrangement by the reaction of aryl / alkyl halide (1a-j) with triethyl phosphite (2) in dry toluene at reflux temperature. Products 3a-j were characterized by IR, 13C and 31P NMR and their antibacterial activity was evaluated.
PREPARATION D'AMINOPHENYL-, NITROPHENYL-, PYRIDYL-, ET QUINOLYLPHOSPHONATES SOUS PHOTOSTIMULATION OU ASSISTANCE METALLIQUE; ACCES AUX ACIDES AMINOPHOSPHONIQUES CORRESPONDANTS
Bulot, J. J.,Aboujaoude, E. Elia,Collignon, N.,Savignac, P.
, p. 197 - 204 (2007/10/02)
Our aim was to study the aromatic nucleophilic substitution between the sodium anion of diethylphosphite and several halogenated substrates like: iodo-anilines, iodo-nitrobenzenes, bromo- and iodopyridines, bromoquinoline.Two coupling processes have been evaluted.The first one is the photostimulated nucleophilic substitution (SRN1), the second the promoted arylation by transition metals.We obtain good results with the first method which is efficient and simple; by contrast the second one has given only few positive results.We describe five aromatic aminophosphonic acids.
