Efficient Solid-Phase Synthesis of Symmetric Norbinaltorphimine Derivatives

<UFIGR ID="ol0351854n00001">We describe an efficient solid-phase synthesis of symmetric norbinaltorphimine (norBNI) derivatives <BO>2</BO>. Pyrrole formation involving the homocoupling of two solid-supported ketones <BO>6</BO>, followed by chemoselective and sequential N-alkylation, provided N-substituted norBNI derivatives <BO>2</BO>. Use of this methodology led to the combinatorial synthesis of 120 norBNI derivatives.