Three pseudopolymorphs based on a coordination complex of a pyrazolyl-benzimidazole ligand have been synthesized and characterized by single crystal X-diffraction, and showed remarkable antibacterial properties.
Three successive and regiocontroled palladium cross-coupling reactions to easily synthesize novel series of 2,4,6-tris(het)aryl pyrido[1 0 ,2 0 :1,5]pyrazolo [3,4-d]pyrimidines †The first access to tris(het)arylated pyrido[1 0 ,2 0 :1,5]pyrazolo [3,4-d]pyrimidine derivatives is reported. The series were generated from 4-chloroaminopyridinium, which afforded the key intermediate bearing three leaving groups, i.e. a C-2 methylsulfanyl, a lactame carbonyl group in C-4 and a chlorine atom in C-6. The regioselective reactions led to the tris(het)aryl derivatives with satisfying to high yields. The three successive cross-coupling reactions occurred first in C-6 by the displacement of chlorine, next in C-4 position by a sequential Pd-catalyzed phosphonium coupling and finally in C-2 under a Pd/Cucatalyzed desulfitative cross-coupling reaction. The optimization and scope of each reaction are discussed and the original compounds characterized.
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