Abstract

Abstract Guanidine derivatives posses a variety of pharmacological activities like fungicidal, antiplasmodial, antibacterial and insect-repelling action; in addition they are suitable starting materials for the preparation of benzodiazaanthracene derivatives2,3. Several methods for the preparation of these compounds have been described; they involve addition of amines to carbodiimides4–7, reaction of thioureas with methyl iodide and amines 8,9, addition of amines to isocyanide dichlorides10 or isocyanide-mercuric chloride complexes11, and by reaction of carbonyl chloride with ureas.12 Most of these procedures posses obvious disadvantages, particularly for the preparation of N,N′, N′-trisubstituted guanidines in view of a mixture of isomeric guanidines are obtained, which are difficult to separate.13

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