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Abstract
AbstractWe describe a general method for metal‐free cyclopropanation of different electron‐deficient olefins with N‐tosylhydrazones as a source of diazo compounds. This method works with N‐tosylhydrazones derived from acetophenones or benzophenones. This reaction is carried out in the presence of LiOtBu as a base to generate diazo species in situ. This method is compatible with various electron‐donating or electron‐withdrawing substituents and allows us to obtain a large library of functionalized tetrasubstituted cyclopropanes. Furthermore, we have used this method to synthesize isocombretastatine A4 analogues, which have submicromolar cytotoxicity against HCT‐116 cell lines.
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