The ruthenium-catalyzed C–H functionalization of enamides with isocyanates: easy entry to pyrimidin-4-ones

Pengfei Shi,^aSong Li,^aLu-Min Hu,^aCong Wang,^aTeck-Peng Loh*^aband Xu-Hong Hu*^a

^aInstitute of Advanced Synthesis, School of Chemistry and Molecular Engineering, Nanjing Tech University, Nanjing 211816, China.

^bDivision of Chemistry and Biological Chemistry, School of Physical and Mathematical Sciences, Nanyang Technological University, Singapore 637371, Singapore.

Abstract:Ruthenium-catalyzed heteroannulation between enamides and isocyanates has been realized as a complementary approach to conventional strategies for the synthesis of pyrimidin-4-ones. High step- and atom-economy was achieved for the rapid construction of such privileged scaffolds, which are found in a multitude of pharmaceutical compounds. The generality and practicability of this transformation were reflected by the broad scope of substrates with diverse functional groups, large-scale synthesis, and late-stage diversification.

Chem. Commun.DOI: 10.1039/c9cc03612a(2018年影响因子：6.164)

论文链接：https://pubs.rsc.org/en/content/articlelanding/2019/cc/c9cc03612a#!divAbstract