Copper-Catalyzed C-N, C-O Coupling Reaction of Arylglyoxylic Acids with Isatins
作者:Rashmi Prakash、Sanjib Gogoi
DOI:10.1002/adsc.201600516
日期:2016.10.6
The copper(II)‐catalyzed decarboxylative couplingreactions of arylglyoxylic acids with isatins afford 4H‐benzo[d][1,3]oxazin‐4‐ones via decarbonylation and concurrent C–N, C–O bond formation.
芳基乙醛酸与Isatin的铜(II)催化的脱羧偶联反应通过脱羰作用和同时的C–N,C–O键形成提供4 H-苯并[ d ] [1,3]恶嗪-4-酮。
One-pot approach to 2-arylbenzoxazinone derivatives from 2-alkynylanilines using copper-mediated tandem reactions
作者:Mitsuaki Yamashita、Akira Iida
DOI:10.1016/j.tet.2014.06.056
日期:2014.9
describe a one-pot method to obtain a variety of 2-arylbenzoxazinones and N-benzoyl anthranilic acid by using a copper catalyst and molecular oxygen as oxidants. This protocol involves tandem cyclization and oxidative processes of 2-alkynylanilines to afford significant motifs in synthetic and medicinal chemistry with moderate yields. We also demonstrated that combining the Sonogashiracoupling and the
A novel and efficient method for the oxidation of 2-arylindoles to synthesize 2-arylbenzoxazinones utilizing oxone as the sole oxidant has been developed. The reaction tolerates a wide range of functional groups and allows quick and atom-economical assembly of a variety of valuable 2-arylbenzoxazinones in high yields.
From Methaqualone and Beyond: Structure–Activity Relationship of 6-, 7-, and 8-Substituted 2,3-Diphenyl-quinazolin-4(3<i>H</i>)-ones and in Silico Prediction of Putative Binding Modes of Quinazolin-4(3<i>H</i>)-ones as Positive Allosteric Modulators of GABA<sub>A</sub> Receptors
作者:Peng-Fei Wang、Anders A. Jensen、Lennart Bunch
DOI:10.1021/acschemneuro.0c00600
日期:2020.12.16
Methaqualone (2-methyl-3-(o-tolyl)-quinazolin-4(3H)-one, MTQ) is a moderately potent positive allostericmodulator (PAM) of GABAA receptors (GABAARs). In a previous structure–activity relationship (SAR) study probing the importance of 2- and 3-substituents in the quinazolin-4(3H)-one scaffold, several potent GABAAR PAMs were identified, including 2,3-diphenylquinazolin-4(3H)-one (PPQ) and 3-(2-chl
甲基苯二甲酮(2-甲基-3-(邻甲苯基)-喹唑啉-4(3 H)-one,MTQ)是GABA A受体(GABA A Rs)的中度有效正变构调节剂(PAM )。在先前的结构-活性关系(SAR)研究中,研究了喹唑啉-4(3 H)-一个支架中2-和3-取代基的重要性,确定了几种有效的GABA A R PAM,包括2,3-二苯基喹唑啉- 4(3 H)-1(PPQ)和3-(2-氯苯基)-2-苯基喹唑啉-4(3 H)-1(Cl-PPQ)。在这里,PPQ被用作喹唑啉4(3 H中的6、7和8个取代基的SAR研究的先导)-通过合成和功能表征36种不同GABA A R亚型的PPQ类似物。尽管没有一个新的类似物比PPQ具有更强的效力或在测试的GABA A Rs上显示出明显的亚型选择性,但从这项研究中提取了一些有趣的SAR观察结果。在一个在硅片的研究中,在跨膜MTQ,PPQ,和Cl-PPQ的推定的结合模式β 2 (+)
Palladium (0)-catalyzed C(sp)-H oxygenation with carboxylic acids
作者:Jia-Yuan Yong、Huu-Manh Vu、Xu-Qin Li、Ai-Jun Gong
DOI:10.1016/j.tet.2020.130969
日期:2020.3
Palladium (0)-catalyzed Ortho-benzoxylation of the sp2 C–H bond of arylbenzoxazinones with carboxylic acid is reported. With benzoxazinone as directing group, the reaction went smoothly under the benign condition and gave the desired product with excellent ortho selectivity. This procedure is compatible with a wide range of functional groups without the use of any ligands or additives. This method