A practical process for the synthesis of translocator protein 18kDa imidazopyridine ligand

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• 作者：Meng Wen (1)
  Chunrong Qu (1)
  Xinhui Su (2)
  Mingmin Ding (1)
  Zixin Deng (1)
  Xuechuan Hong (1)
  
• 关键词：translocatorprotein 18kDa (TSPO) ; synthesis ; imidazopyridine ; activated copper ; antitumor ; O 62
• 刊名：Wuhan University Journal of Natural Sciences
• 出版年：2014
• 出版时间：February 2014
• 年：2014
• 卷：19
• 期：1
• 页码：19-26
• 全文大小：509 KB
• 作者单位：Meng Wen (1)
  Chunrong Qu (1)
  Xinhui Su (2)
  Mingmin Ding (1)
  Zixin Deng (1)
  Xuechuan Hong (1)
  
  1. Key Laboratory of Combinatorial Biosynthesis and Drug Discovery of Ministry of Education/School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, Hubei, China
  2. Department of Nuclear Medicine and Minnan PET Center, the First Affiliated Hospital, Xiamen University, Xiamen, 361003, Fujian, China
  
• ISSN：1993-4998

文摘

In this article, an effective feasible method to synthesize translocator protein 18kDa (TSPO) imidazopyridine ligand 7 is discussed. A new procedure for the synthesis of the key intermediate 17 has been developed in four steps (condensation, diazo reaction, hydrolysis, amidation) from 2-aminopyridine 18. The overall yield was increased from 18% to 31.6%. One of the key steps is using activated copper powder as a catalyst in several cycles. Finally, reduction of 17 with Zn dust completed the synthesis of TSPO imidazopyridine ligand 7 in 86% yield.