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吡唑并[4′,3′:5,6]吡喃并[2,3-d]嘧啶化合物的合成与生物活性

刘建超 任青云 贺红武

应用化学2017,Vol.34Issue(11):1279-1286,8.
应用化学2017,Vol.34Issue(11):1279-1286,8.DOI:10.11944/j.issn.1000-0518.2017.11.160502

吡唑并[4′,3′:5,6]吡喃并[2,3-d]嘧啶化合物的合成与生物活性

Synthesis and Biological Activity of Pyrazolo[4′,3′:5,6]pyrano[2,3-d]pyrimidine Derivatives

刘建超 1任青云 2贺红武1

作者信息

  • 1. 华中师范大学化学学院 武汉430079
  • 2. 广东东阳光药业研究院新药所抗感染原创部 广东东莞523871
  • 折叠

摘要

Abstract

A series of new 2-substituted-3 ,8-diphenyl-5-aryl-6-methyl-5 ,8-dihydropyrazolo [4′,3′:5 ,6 ] pyrano[2,3-d ]pyrimidine derivatives was designed and synthesized via tandem aza-Wittig reaction. The structures of target compounds were confirmed by 1 H NMR,IR spectra and elemental analysis. The structure of 2-dipropylamino-3,8-diphenyl-5-(4-methylphenyl)-6-methyl-5,8-dihydropyrazolo[4′,3′:5,6]pyrano[2,3-d]pyrimidin-4(3H)-one was determined by single crystal X-ray diffraction. The results of preliminary bioassay indicate that some compounds possess good inhibition activities against Botrytis cinereapers at a dosage of 5. 0 × 10 -5 g/mL,and the inhibition rates against Botrytis cinereapers are above 90%. Target compounds possess no insecticidal activity against Nilaparvatalegen, but show obvious insecticidal activity against Mythimaseparata,and the inhibihition rates against Mythimaseparata are above 60%.

关键词

氮杂Wittig反应/吡唑并嘧啶/吡喃并嘧啶/生物活性

Key words

Aza-Wittig reaction/pyrazolopyrimidine/pyranopyrimidine/biological activity

分类

化学化工

引用本文复制引用

刘建超,任青云,贺红武..吡唑并[4′,3′:5,6]吡喃并[2,3-d]嘧啶化合物的合成与生物活性[J].应用化学,2017,34(11):1279-1286,8.

基金项目

国家自然科学基金(21172090,31000867)、教育部创新团队(IRT0953)资助 (21172090,31000867)

Supported by the National Natural Science Fundation of China(No. 21172090,No. 31000867),the Program for Changjiang Scholars and Innovatives Research Team in University(No. IRT0953) (No. 21172090,No. 31000867)

应用化学

OA北大核心CSCDCSTPCD

1000-0518

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