Synthesis of Apomorphine Analogues by the Intermolecular Benzyne Cycloaddition (IBC) Approach.

Abstract A highly convergent, regioselective synthesis of apomorphine analogues is described. It relies on the intermolecular cycloaddition between a 1-methylene-1,2,3,4-tetrahydroisoquinoline and an asymmetrically substituted aryne.