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Protocol for Sonogashira coupling of alkynes and aryl halides via nickel catalysis
Hui Chen1, Zhenkang Ai1, Xuebin Liao1
1School of Pharmaceutical Sciences, State Key Laboratory of Molecular Oncology, Tsinghua-Peking Center for Life Science, Tsinghua University, Beijing 100084, China.
Abstract:
Alkynes are widely present in natural products and pharmaceutical compounds. Here, we present a protocol for nickel-catalyzed cross-coupling of terminal alkynes with aryl iodides or bromides for constructing a C(sp2)-C(sp) bond. We describe steps for reagent preparation, reaction setup, purification process, and product characterization. We also detail procedures for obtaining a single crystal of 6-(phenylethynyl)-1-(phenylsulfonyl)-1H-indole (3b). The application of this protocol is limited to aryl bromide and iodide. For complete details on the use and execution of this protocol, please refer to Chen et al.1.
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