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Updated: Apr 22, 2026

A Direct, Early Stage Guanidinylation Protocol for the Synthesis of Complex Aminoguanidine-containing Natural Products
Published on: September 9, 2016
Recent development of synthetic preparation methods for guanidines via transition metal catalysis
Wen-Xiong Zhang1, Ling Xu, Zhenfeng Xi
1Beijing National Laboratory for Molecular Sciences, and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry, Peking University, Beijing 100871, China. wx_zhang@pku.edu.cn.
Abstract:
Multisubstituted guanidines have received much attention because of important applications in many fields, such as pharmaceutics, organometallic and coordination chemistry, and organic synthesis. Although classical methods are available for the preparation of guanidines, synthetic preparation approaches to guanidines are still in great demand. In this review, we summarize recent developments on synthetic methods via the C-N bond formation. Three aspects are included: transition-metal-catalyzed guanidine synthesis based on classical methods; catalytic guanylation reaction of amines with carbodiimides; and tandem catalytic guanylation/cyclization reactions.
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