• 文献标题:   Sulphonated graphene oxide catalyzed continuous flow synthesis of pyrazolo pyrimidinones, sildenafil and other PDE-5 inhibitors
  • 文献类型:   Article
  • 作  者:   STHALAM VK, MAHAJAN B, KARRA PR, SINGH AK, PABBARAJA S
  • 作者关键词:  
  • 出版物名称:   RSC ADVANCES
  • ISSN:  
  • 通讯作者地址:  
  • 被引频次:   3
  • DOI:   10.1039/d1ra08220e
  • 出版年:   2021

▎ 摘  要

Sulphonated graphene oxide was used for cascade condensation and cyclization reactions towards accessing substituted pyrazolo pyrimidinones. Further, sulphonation and amination reactions were integrated through continuous flow chemistry to access PDE-5 inhibitors. Herein, we report a simple continuous synthetic platform that reduce tedious manual operations and accelerate the synthesis of several potent inhibitors of phosphodiesterase type-5. The developed platform enabled us to perform one-flow multi-step, multi-operational process to synthesize the PDE-5 inhibitors such as sildenafil and its analogues in 32.3 min of the reaction time, with minimal human intervention and single solvent.