Synthesis And Application Of α-substituted Monothiomalonates And β-thioester Weinreb Amide

A new method for the preparation of α-substituted mono-thiolmalonate and β-thioler-Weinreb amides was developed by direct acylation of thiolesters at α sites using simple thiolesters as substrates,enolation under soft and hard conditions and oxyimidazole and imidazole Weinreb amides as acylation reagents.Both methods have the advantages of mild conditions and simple post-treatment,and high yield products were obtained under "hard" conditions.In addition,α-substituted mono-thiolmalonate and β-thiolester-Weinreb amide were transformed into potential bioactive molecules such as indoleone containing quaternary carbon centers.