Chin. J. Org. Chem. ›› 2008, Vol. 28 ›› Issue (09): 1598-1604. Previous Articles     Next Articles

Original Articles


李海涛; 刘 河*; 李 伟 ; 仲伯华   

  1. (军事医学科学院毒物药物研究所 北京 100850)
  • 收稿日期:2008-02-04 修回日期:2008-03-28 发布日期:2008-09-20
  • 通讯作者: 刘 河

Design and Synthesis of Aroyl Pyrrolizine Derivatives

LI, Hai-Tao; LIU, He* ; LI, Wei ; ZHONG, Bo-Hua   

  1. (Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850)
  • Received:2008-02-04 Revised:2008-03-28 Published:2008-09-20
  • Contact: LIU, He

Dual inhibitors of COX and 5-LOX may have synergistic anti-inflammatory effects and reduce the side-effects of COX inhibitors by blocking the formation of both prostaglandins and leucotrienes. In this paper, two series of compounds with pyrrolizine as a template were designed and synthesized as novel COX/5-LOX dual inhibitors, including 5-aroyl-7-aryl-2,3-dihydro-1H-pyrrolizines and 6-aroyl-7-aryl-2,3- dihydro-1H-pyrrolizines, and an efficient synthetic method has been developed for the synthesis of 5- or 6-aroylpyrrolizine. All target compounds have been identified by MS, 1H NMR spectra and elemental analy-sis. The structures and molecular configuration of compound III and IV have been confirmed by NMR spectra.

Key words: pyrrolizine derivative, synthesis, non-steroidal anti-inflammatory drug