Rapid and efficient Pd-catalyzed Sonogashira coupling of aryl chlorides.
An efficient and effective microwave-assisted cross-coupling of terminal alkynes with various aryl chlorides including sterically hindered, electron-rich, electron-neutral, and electron-deficient aryl chloride is developed. It proceeds faster and generally gives good to excellent yields and also can be extended successfully to the Suzuki coupling and Buchwald-Hartwig amination, as well as the Heck coupling with inert aryl chlorides. The short reaction times and simple reaction conditions coupling with a broad substrate scope render this method particularly attractive for the efficient preparation of biologically and medicinally interesting molecules.
Huang
He
H
Drug Discovery and Design Centre, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, and Graduate School, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China.
Liu
Hong
H
Jiang
Hualiang
H
Chen
Kaixian
K
D000114:Acetylene / Q000737:chemistry; D000480:Alkynes / Q000737:chemistry; D002384:Catalysis; D002712:Chlorides / Q000737:chemistry*; D008745:Methylation; D008872:Microwaves; D015394:Molecular Structure; D010165:Palladium / Q000737:chemistry*; D013237:Stereoisomerism; D013997:Time Factors
D000480:Alkynes; D002712:Chlorides; D010165:Palladium; D000114:Acetylene