174422-22-1Relevant articles and documents
3D-Printed Polypropylene Continuous-Flow Column Reactors: Exploration of Reactor Utility in SNAr Reactions and the Synthesis of Bicyclic and Tetracyclic Heterocycles
Rao, Zenobia X.,Patel, Bhaven,Monaco, Alessandra,Cao, Zi Jing,Barniol-Xicota, Marta,Pichon, Enora,Ladlow, Mark,Hilton, Stephen T.
supporting information, p. 6499 - 6504 (2017/09/25)
3D printing has the potential to transform the way in which chemical reactions are carried out due to its low-cost, ease-of-use as a technology and its capacity to expedite the development of iteratively enhanced prototypes. In this present study, we developed a novel, low-cost polypropylene (PP) column reactor that was incorporated into an existing continuous-flow reactor for the synthesis of heterocycles. The utility and solvent resistance of the printed devices were explored in SNAr reactions to produce substituted aniline derivatives and in the synthesis of bicyclic and tetracyclic heterocycles. Using this approach, a range of heterocyclic compounds was synthesised including the core structure of the natural product (±)-γ-lycorane and structurally complex compounds based on the tetracyclic core of the erythrina alkaloids.
NOVEL HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
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Paragraph 0419, (2013/06/28)
The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compoun
Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist
Sime, Mairi,Allan, Amanda C.,Chapman, Paul,Fieldhouse, Charlotte,Giblin, Gerard M.P.,Healy, Mark P.,Lambert, Millard H.,Leesnitzer, Lisa M.,Lewis, Ann,Merrihew, Raymond V.,Rutter, Richard A.,Sasse, Rosemary,Shearer, Barry G.,Wilson, Timothy M.,Xu, Robert X.,Virley, David J.
scheme or table, p. 5568 - 5572 (2011/10/09)
The peroxisome proliferator-activated receptor γ (PPARγ) is a ligand-activated nuclear receptor, thought to play a role in energy metabolism, glucose homeostasis and microglia-mediated neuroinflammation. A novel benzimidazole series of centrally penetrant PPARγ partial agonists has been identified. The optimization of PPARγ activity and in vivo pharmacokinetics leading to the identification of GSK1997132B a potent, metabolically stable and centrally penetrant PPARγ partial agonist, is described.