Aged red wine pigments as a source of inspiration for organic synthesis—the cases of the color-stable pyranoflavylium and flavylium-(4→8)-flavan chromophores
摘要:
Two flavylium-based chromophores peculiar to aged red wine pigments are investigated from a synthetic viewpoint. The condensation between easy-to-prepare 5-hydroxy-4-methylflavylium salts and aldehydes, giving birth to color-stable pyranoflavylium pigments, further proves efficient and wide in scope. A set of some twenty structurally-related flavylium-based pigments has been prepared and structure:color relationships are discussed. Furthermore, the synthesis of the flavylium-(4 -> 8)-flavan chromophore is achieved via a novel three-step sequence. The elaborated sequence starts with an iodine magnesium exchange from an 8-iodinated flavan, thus generating a magnesiated species that then smoothly reacts with a flavone to furnish an adduct, that finally leads to the expected chromophore via dehydration. (C) 2014 Elsevier Ltd. All rights reserved.
[EN] THIENO-PYRIDINONE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] UTILISATION DE DERIVES DE THIENO-PYRIDONONE COMME INHIBITEURS DE KINASES
申请人:CELLTECH R&D LTD
公开号:WO2005042540A1
公开(公告)日:2005-05-12
A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 3-position by an arylcarbonyl or heteroarylcarbonyl moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.
new strategy for the synthesis of 3-arylisocoumarins and 8-hydroxy-3-arylisocoumarins was investigated by using acylanion chemistry for the initial C–C bond formation. The obtained keto esters and keto lactones as intermediates underwent based-promoted intramolecular cyclization to afford 3-arylisocoumarins in good yields. The developed methodology was applied for the synthesis of the important natural
3-芳基异香豆素和8-羟基-3-芳基异香豆素的合成新策略通过使用酰基阴离子化学进行初始C-C键形成研究。得到的酮酯和酮内酯作为中间体进行基于促进的分子内环化,以良好的产率得到3-芳基异香豆素。所开发的方法用于合成重要的天然产物 thunberginol A 和 cajanolactone A。
A Defunctionalization Concept for the Convenient Synthesis of Bis(5-arylfuran-2-yl)methane Scaffolds
The bis(5-arylfuran-2-yl)methane framework has been obtained through defunctionalization of aryl ketones, derived from abundantly available L-(+)-tartaric acid, under the influence of acid. The stereocomponents present in these starting aryl ketones have been found to be insignificant for this transformation.
A nitrile-stabilized ammonium ylide as a masked C–CN synthon in heterocyclization with amidine–imine: 3-component assembly to fused pyrimidine scaffolds
作者:Sankar K. Guchhait、Meenu Saini、Divyani Sumkaria、Vikas Chaudhary
DOI:10.1039/c7cc02946b
日期:——
nitrile-stabilized quaternary ammonium ylide as masked C–C=N synthon in contrast to its usual sigmatropic rearrangement has been demonstrated. Its reaction with 2-aminopyridine-derived aldimine undergoes electronically-assisted nucleophilic additions and Hofmannelimination, and provides a new method to access fused-pyrimidines.
Thieno-pyridinone derivatives as kinase inhibitors
申请人:Alexander Peter Rikki
公开号:US20070078131A1
公开(公告)日:2007-04-05
A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 3-position by an arylcarbonyl or heteroaryl-carbonyl moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.