Syntheses of Combretastatin A‐4 and Related Stilbenes by Using Aqueous Conditions

Combretastatin A-4 (CA4) is a potent anti-mitotic and vascular disrupting agent. Organic chemists have been working to optimize the synthesis of CA4 for past 3 decades, with methods requiring hazardous solvents harsh reaction conditions. Here, we report variety stilbenes in an aqueous Wittig system. Potassium carbonate or lithium hydroxide were used as base this give excellent yields mixtures E- Z-stilbenes. The was achieved using tetrahydropyran (THP) silyl protected phenolic aldehydes. THP groups removed dilute acid whilst fortuitously fell off during work up.