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Late-Stage C-H Arylation of Thiazolo[5,4- f ]quinazolin-9(8 H)-one Backbone: Synthesis of an Array of Potential Kinase Inhibitors

Abstract : Driven by the need of structural modification to establish structure-activity relationships, the regioselective C–H bond activation of thiazolo[5,4-f]quinazolin-9(8H)-one backbone has been developed to furnish the corresponding C2-arylated valuable scaffold. This strategy provides a synthetically streamlined and useful route for late-stage diversification of this attractive skeleton, required in drug discovery. A more eco-friendly synthesis of thiazolo[5,4-f]quinazolin-9(8H)-ones is also described giving access to these aforementioned compounds in a facile manner.
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https://hal-normandie-univ.archives-ouvertes.fr/hal-02046272
Contributor : Madeleine Roux-Merlin <>
Submitted on : Friday, February 22, 2019 - 3:39:40 PM
Last modification on : Thursday, July 2, 2020 - 3:28:42 AM

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Florence Couly, Carole Dubouilh-Benard, Thierry Besson, Corinne Fruit. Late-Stage C-H Arylation of Thiazolo[5,4- f ]quinazolin-9(8 H)-one Backbone: Synthesis of an Array of Potential Kinase Inhibitors. SYNTHESIS, Georg Thieme Verlag, 2017, 49 (20), pp.4615-4622. ⟨10.1055/s-0036-1588434⟩. ⟨hal-02046272⟩

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