Abstract
The new three-component Biginelli reaction of aromatic isocyanate, ethyl acetoacetate, and substituted urea (or thiourea as well as guanidine) is described for the first time. In this reaction, N 4-aryl-5-carboxyl-6-methyl cytimidine derivatives were obtained in moderate to excellent yields by employing DBU as a highly effective catalyst. This methodology provides several advantages such as good functional group tolerance, excellent yields, atom efficiency, and experimental simplicity.
GRAPHICAL ABSTRACT
ACKNOWLEDGMENTS
We thank Dr. Biing-Jiun Uang from National Tsing Hua University and Dr. Qixing Zhong from National University of Singapore for their generous assistance in the preparation of this manuscript. We appreciate the support from Center for Instrumental Analysis, China Pharmaceutical University, for their contribution in the structural confirmation.