Abstract

A synthetic route to ecteinascidin 743 has been established via an intramolecular cascade Heck reaction to construct the diazabicyclo[3.3.1]nonane skeleton while controlling the two contiguous stereogenic centers. The strategically formed five-membered ring was oxidatively cleaved to generate a dialdehyde intermediate, from which the B ring of ecteinascidin 743 was constructed.

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