An efficient synthesis of 4,6-substituted pyrrolo[3,2-d]pyrimidines by silver-catalyzed cyclization of acetylene amine

作者：Xie, Rui; Hu, Ying; Wan, Huixin; Hu, Yanwei^*; Chen, Shaohua; Zhang, Shilei^*; Zhang, Yinan^*

来源：Tetrahedron Letters, 2016, 57(22): 2418-2421.

DOI：10.1016/j.tetlet.2016.04.077

• Heterocycles
• Transition-metal catalysts
• Cyclization
• Bioactive molecules

A silver catalyzed cyclization of acetylene amine was developed to synthesize 4,6-substituted pyrrolo [3,2-d]pyrimidine, a bioactive isosteric scaffold of purine. Starting from simple commercially available acetylenes and pyrimidines, the method was found to be compatible with wide chemical functionalities, leading to a series of pyrrolo[3,2-d]pyrimidines in 84-91% yields. 2016 Elsevier Ltd.

• 出版日期2016-6-1
• 单位苏州大学