Abstract
A library of C2-arylated pyrrolo[2,1-c][1,4]benzodiazepines (PDB) was prepared through the Suzuki-Miyaura coupling of vinyl triflate 1 using a PS-supported palladium catalyst. Parallel reactions of the Suzuki-Miyaura coupling of 1 with a diverse set of boron reagents (66 examples) were carried out with a PS-supported palladium-phosphine complex under microwave conditions. After completion of the coupling reactions, N,N-diethanolaminomethyl polystyrene (PS-DEAM) was added to each reaction mixture to trap the unreacted boron reagent. The resulting mixtures were then subjected to parallel filtration through a phase separator cartridge to isolate the Suzuki products 2.
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