Microwave assisted unprotected Sonogashira reaction in water for the synthesis of multi-replaced aromatic acetylene compounds

A microwave-assisted, efficient and rapid Sonogashira reaction was developed for the synthesis of polysubstituted aromatic alkynes. The reaction was environmentally friendly and easy to handle by replacing traditional amine solvents with water. The optimized reaction conditions could obtain the products with high yields, while reducing the dependence on anaerobic reaction conditions with no inert gas protection. The reaction can also achieve milligram level, overcoming the problem of TMSA volatilization in a small amount of reaction. The environmentally friendly reaction solvent, mild reaction conditions, high reaction yields and short reaction time made the reaction a method of highly promising application, especially in synthesizing porous aromatic frameworks.