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A concise/catalytic approach for the construction of the C14-C28 fragment of eribulin.

Sibadatta SenapatiChepuri V Ramana
Published in: Organic & biomolecular chemistry (2022)
A simple approach for the synthesis of the C14-C28 fragment of eribulin has been developed by employing a one-pot gold-catalyzed alkynol cyclization/Kishi reduction to construct the 1,5-cis-tetrahydropyran unit and a cross-metathesis/Sharpless asymmetric dihydroxylation-cycloetherification to install the 1,4-trans-tetrahydrofuran ring. Use of easily accessible building blocks, ease of operation and catalytic transformations as key reactions for the construction of THF/THP units highlight the current approach.
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