Synthetic Study of Aquayamycin. Part 3. First Total Synthesis.

Abstract The first total synthesis of aquayamycin (1) has been accomplished. The crucial steps include (1) the Hauser reaction between 3-(phenylsulfonyl)phthalide 3 and cyclohexenone 4 to make up the linear BCD tricycle, and (2) the intramolecular pinacol coupling of keto aldehyde 7 to the full tetracyclic framework.