Journal
CHEMICAL COMMUNICATIONS
Volume 58, Issue 46, Pages 6661-6664Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d2cc01944b
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Funding
- National Natural Science Foundation of China [91956113]
- China Postdoctoral Science Foundation [2021M692152]
- Science and Technology Commission of Shanghai Municipality [20XD1423400, 21ZR1482100, 22ZR1458900]
- Shanghai Municipal Education Commission [2019-01-07-00-10-E00072]
- Shanghai Frontiers Science Center for Traditional Chinese Medicine Chemical Biology
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A new method for traceless directing cross-coupling of unreactive C(sp(3))-H bonds and azole C(sp(2))-H bonds has been described. The success of this cascade process relies on the careful selection of a bulky and electron-rich phosphine ligand, and it offers broad substrate scope, excellent regioselectivity, and good functional group tolerance.
A palladium-catalyzed intermolecular cross-coupling of unreactive C(sp(3))-H bonds and azole C(sp(2))-H bonds with bromide as a traceless directing group is described. The judicious selection of the bulky and electron-rich phosphine ligand is the key for the success of this cascade process. The protocol features a broad substrate scope, excellent regioselectivity, and good functional group tolerance.
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