Abstract
AbstractAn ‘on‐water’ protocol has been developed for the synthesis of combretastatin A‐4 (CA‐4) analogues by cyclization of polarized triaryldivinyl ketones using hydrochloric acid as a promoter in 45–95% yields. The reaction time was reduced by about 30 times due to ultrasonic irradiation at ambient temperature. The other advantages of this new method are operational simplicity, easy workup, no column purification, and applicability on a gram‐scale. It was shown that the amphiphilicity of the substrate and a low energy barrier of the reaction are a prerequisite for electrophilic and concerted reactions under aqueous and ambient conditions.magnified image
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