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6‐Deoxyisojacareubin was directly synthesized in a six‐step route with an overall yield of about 20%. In this route, the excellent site selectivity of this Claisen rearrangement‐cyclization reaction cascade was achieved by inserting a bulky p‐tosyl group into the free 1‐OH, and in the last step, some efficient demethylation methods were explored. Furthermore, all synthesized intermediates including...
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