芳基
氟化物
氟
磷化氢
催化作用
试剂
钯
化学
取代基
组合化学
配体(生物化学)
药物化学
有机化学
无机化学
生物化学
受体
烷基
作者
Donald A. Watson,Mingjuan Su,Georgiy Teverovskiy,Yong Zhang,Jorge García‐Fortanet,Tom Kinzel,Stephen L. Buchwald
出处
期刊:Science
[American Association for the Advancement of Science]
日期:2009-08-14
卷期号:325 (5948): 1661-1664
被引量:615
标识
DOI:10.1126/science.1178239
摘要
Facile Fluorination Fluorine atoms have become a useful substituent in pharmaceuticals. However, they remain challenging to introduce synthetically because present methods for carbon-fluorine bond formation require either corrosive conditions or somewhat exotic, and thus expensive, reagents. A sticking point has been the failure of traditional palladium catalysts to couple aryl groups with coordinated fluoride. Watson et al. (p. 1661 , published online 13 August; see the Perspective by Gouverneur ) show that pairing palladium with a well-designed phosphine ligand produces a versatile catalyst for aryl fluorination using simple fluoride salts. The method tolerates a range of functional groups and should facilitate efficient syntheses of multiple fluoroaromatic targets.
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