1875-58-7Relevant academic research and scientific papers
Nickel-Catalyzed N -Arylation of Amides with (Hetero)aryl Electrophiles by Using a DBU/NaTFA Dual-Base System
Lundrigan, Travis,Tassone, Joseph P.,Stradiotto, Mark
supporting information, p. 1665 - 1669 (2021/01/25)
The first nickel-catalyzed N -arylation of amides with (hetero)aryl (pseudo)halides employing an organic amine base is described. By using a bis(cyclooctadienyl)nickel/8-[2-(dicyclohexylphosphinyl)phenyl]-1,3,5,7-tetramethyl-2,4,6-trioxa-8-phosphaadamantane catalyst mixture in combination with DBU/NaTFA as a dual-base system, a diversity of (hetero)aryl chloride, bromide, tosylate, and mesylate electrophiles were successfully cross-coupled with structurally diverse primary amides, as well as a selection of secondary amide, lactam, and oxazolidone nucleophiles.
Synthesis and trypanocidal activity of substituted 2,4-diarylquinoline derivatives
Oluwafemi, Kola A.,Phunguphungu, Siyolise,Gqunu, Sinalo,Isaacs, Michelle,Hoppe, Heinrich C.,Klein, Rosalyn,Kaye, Perry T.
, (2021/06/17)
A small library of nine, novel 2,4-diarylquinoline derivatives has been prepared in high yield via convenient one-or two-step routes from a series of substituted 2-Aminobenzophenones. None of the products exhibited toxicity at 20 uM against human cervix a
4-aminoquinoline compound, and preparation method and application thereof
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Paragraph 0032-0037, (2019/11/12)
The invention discloses a 4-aminoquinoline compound, and a preparation method and application thereof. The second site of the 4-aminoquinoline compound is replaced by cyclic R-base, the 4-aminoquinoline compound is obtained by 4-step reaction of anthranil
Selective Oxidative Decarbonylative Cleavage of Unstrained C(sp3)-C(sp2) Bond: Synthesis of Substituted Benzoxazinones
Verma, Ajay,Kumar, Sangit
supporting information, p. 4388 - 4391 (2016/10/11)
A transition metal (TM)-free practical synthesis of biologically relevant benzoxazinones has been established via a selective oxidative decarbonylative cleavage of an unstrained C(sp3)-C(sp2) bond employing iodine, sodium bicarbonate, and tbutyl hydroperoxide in DMSO at 95 °C. Control experiments and Density Functional Theory (DFT) calculations suggest that the reaction involves a [1,5]H shift and extrusion of CO gas as the key steps. The extrusion of CO has also been established using PMA-PdCl2.
N-Bu4NI-catalyzed selective dual amination of sp3 C-H bonds: Oxidative domino synthesis of imidazo[1,5-c]quinazolines on a gram-scale
Zhao, Dan,Wang, Teng,Shen, Qi,Li, Jian-Xin
supporting information, p. 4302 - 4304 (2014/04/17)
An n-Bu4NI catalyzed domino reaction that involves selective dual amination of sp3 C-H bonds has been developed. The protocol affords a facile and efficient approach to the synthesis of imidazo[1,5-c] quinazolines under mild conditions.
Evaluation of synthetic acridones and 4-quinolinones as potent inhibitors of cathepsins L and v
Marques, Emerson F.,Bueno, Mauro A.,Duarte, Patricia D.,Silva, Larissa R.S.P.,Martinelli, Ariani M.,Dos Santos, Caio Y.,Severino, Richele P.,Broemme, Dieter,Vieira, Paulo C.,Correa, Arlene G.
experimental part, p. 10 - 21 (2012/08/28)
Cathepsins, also known as lysosomal cysteine peptidases, are members of the papain-like peptidase family, involved in different physiological processes. In addition, cathepsins are implicated in many pathological conditions. This report describes the synthesis and evaluation of a series of N-arylanthranilic acids, acridones, and 4-quinolinones as inhibitors of cathepsins V and L. The kinetics revealed that compounds of the classes of acridones are reversible competitive inhibitors of the target enzyme with affinities in the low micromolar range. They represent promising lead candidates for the discovery of novel competitive cathepsin inhibitors with enhanced selectivity and potency. On the other hand, 4-quinolinones were noncompetitive inhibitors and N-arylanthranilic acids were uncompetitive inhibitors.
