Abstract
A convergent aromatic annulation strategy based on the Michael addition of the dimethyl 1-allyl-1,3-acetonedicarboxylate anion 8 to 4-pivaloyloxy-2-butynal 9, followed by a regiocontrolled Dieckmann-type cyclization over the adequate methyl ester group, has been applied to an efficient formal synthesis of the antitumor antibiotic, mycophenolic acid 1. This tandem annulation reaction generates the fully substituted aromatic intermediate 12, which was transformed by a simple six-step sequence to 2, and even to 1 by the methodology of Birch et al.[15]
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