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A sequential one-pot approach towards N,N'-disubstituted guanidines from N-chlorophthalimide, isocyanides and amines is reported. This strategy provides straightforward and efficient access to diverse guanidines in yields up to 81% through previously unprecedented N-phthaloylguanidines. This protocol also features wide substrate scope and mild conditions.

organic and biomolecular chemistry

One-pot synthesis of diverseN,N′-disubstituted guanidines fromN-chlorophthalimide, isocyanides and aminesvia N-phthaloyl-guanidines