ARTICLES

An Efficient and Rapid Synthesis of 1H-Pyrazolo[3,4-d]-pyrimidin-4(5H)-one in Water

  • Ziqi Su ,
  • Qi Zhang ,
  • Jieqiang Zhao ,
  • Tao Zhao ,
  • Wenyi Liu ,
  • Huiping Wang ,
  • Juan Xu ,
  • Jiarong Li
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  • a School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing 102488
    b National Research Institute for Family Planning, Beijing 100081
* Corresponding authors. E-mail: ;

Received date: 2021-04-19

  Revised date: 2021-05-10

  Online published: 2021-06-08

Supported by

Chinese Academy of Medical Sciences Innovation Fund for Medical Sciences(2018-I2M-1-004); Non-profit Central Research Institute Fund of National Research Institute for Family Planing(2021GJZ05)

Abstract

Abstract Pyrazolopyrimidinone compounds have many biological activities and been widely used due to the similar structure of purines in organisms. However, the traditional synthetic methods suffered from several drawbacks, such as acylation and cyclization. Herein, one pot cyclization of 1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one was developed by one pot conversion of 5-amino-4-cyano-pyrazole and aromatic aldehydes in the presence of sodium hydroxide using water as media. The reaction was carried out under the conditions of easily available raw materials, simple operation, and showed good tolerance to various functional groups.

Cite this article

Ziqi Su , Qi Zhang , Jieqiang Zhao , Tao Zhao , Wenyi Liu , Huiping Wang , Juan Xu , Jiarong Li . An Efficient and Rapid Synthesis of 1H-Pyrazolo[3,4-d]-pyrimidin-4(5H)-one in Water[J]. Chinese Journal of Organic Chemistry, 2021 , 41(9) : 3701 -3709 . DOI: 10.6023/cjoc202104043

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