Synthesis of α-cyanato-α′-carbonyl sulfoxonium ylides in water

A new strategy for direct access to unreported α-cyanato-α′-carbonyl sulfoxonium ylides is reported. The developed open-flask operation is a catalyst-, metal- and additive-free green process, which has good compatibility with various substituents and generally excellent yields. This protocol can be applied to gram-scale production and modification of bioactive drugs which demonstrate the practicality of this method. A new catalyst-, metal- and additive-free green strategy to synthesize bis-substituted sulfoxonium ylides is reported, which has good compatibility with various substituents and generally excellent yields.