Transition Metal‐Free Synthesis of 3‐Alkynylpyrrole‐2‐carboxylates via Michael Addition/Intramolecular Cyclodehydration

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Abstract
A transition metal‐free and efficient method for the synthesis of 3‐alkynylpyrrole‐2‐carboxylates from diynones and glycine esters or 2‐aminoacetophenone hydrochloride has been developed. This transformation provides a large range of substituted pyrroles in good to excellent yields with the elimination of water as the only by‐product. The detailed mechanistic studies elucidated that this transformation involves a Michael addition/intramolecular cyclodehydration process. magnified image
Funding Information
  • Ministry of Education of China (IRT1225)
  • National Natural Science Foundation of China (21362002, 41465009 and 81260472)
  • Guangxi Natural Science Foundation of China (2014GXNSFDA118007)
  • State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources (CMEMR2014A02 and CMEMR2012A20)
  • BAGUI Scholar Program

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