Abstract

Abstract In this study, the concise total synthesis of crambescin B methyl ester, a cyclic guanidine alkaloid, has been achieved. The key aspects of this new approach include: 1) A Mannich reaction between α-amidosulfone and β-ketoester to construct the main scaffold and 2) Acid-catalyzed dehydrative cyclization leading to enol ether in a highly stereoselective manner. The synthetic approach reported herein is nine steps shorter than our previously published method.

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