The synthetic progress of bioactive 2,7'-cyclolignans is reviewed. After a short introduction to biosynthesis and chemoenzymatic synthesis, the chemical synthesis of various aryltetralin, dihydronaphthalene and 7'-arylnaphthalene-types of these lignans is demonstrated. Notably, newly developed methods, such as Pd-catalyzed C-H arylation, organocatalysis and photocatalysis under visible-light, are discussed during the construction of their skeleton.
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