![Mizoroki-Heck Cross-coupling Reactions Catalyzed by Dichloro{bis[1,1',1''-phosphinetriyltripiperidine]}palladium Under Mild Reaction Conditions](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F51444.jpg&w=3840&q=50)
Access to Terminal Alkynes via Palladium-Catalyzed Coupling of ArCl with a Low Catalyst Loading of 0.08 mol
Lei Xu1, Gen-Qiang Chen2, Xumu Zhang1,2,3
1Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis, Department of Chemistry and Medi-X Pingshan, Southern University of Science and Technology, Shenzhen 518055, People's Republic of China.
None:
The synthesis of terminal alkynes from inexpensive aryl chlorides remains a challenging task in organic synthesis. Here, a Heck-Cassar reaction of aryl chlorides with (triisopropylsilyl)acetylene catalyzed by low loadings of palladium (0.08 mol %) has been developed. Through subsequent desilylation, aryl-substituted terminal alkynes can be readily prepared. This reaction features robustness and good functional group compatibility, making it suitable for the late-stage modification of drug molecules.
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