Journal
SYNTHESIS-STUTTGART
Volume 53, Issue 7, Pages 1356-1364Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0040-1707329
Keywords
4-arylquinazolines; palladium(II) catalysis; one-pot assembly; tandem cyclization reaction; ligands
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Funding
- National Key Research and Development Program of China [2017YFE0102200]
- National Natural Science Foundation of China [81673291]
- Diabetes National Research Group, USA
- Natural Science Foundation of Zhejiang Province [LY18H300001]
- Multiple Sclerosis National Research Institute, USA
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The study presents a one-pot method for joining three separate components to produce a variety of 4-arylquinazolines in good to excellent yields. The method involves a palladium(II)-catalyzed cascade reaction that can be easily scaled up and applied to the synthesis of a translocator protein (TSPO) ligand.
A one-pot method for joining three separate components leading to an assortment of 4-arylquinazolines (27 examples) in good to excellent yields is described. The method consists of a palladium(II)-catalyzed- cascade reaction involving C(sp)-C(sp(2)) coupling followed by intramolecular C-N bond formation. The reaction was readily scaled up to gram quantity and successfully applied to the synthesis of a translocator- protein (TSPO) ligand.
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