Abstract
Abstract The new and versatile method for the synthesis of integrastatin core has been developed by the use of o-toluic acid and 2′-hydroxyacetophenone with NaH/sec-BuLi, followed by the reaction of dihydroisocoumarins with MeLi. The overall steps for the synthesis of integrastatin core was only 3 steps including the known method by the literature. The scope and limitations of substrates bearing the various substituents on the aromatic ring were investigated. The chemical yields by our approach are generally high and the current route enables us the rapid synthesis.
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