有机化学ChineseJournalofOrganicChemistryARTICLE*Correspondingauthors.E-mail:liuyan@shzu.edu.cn;liuping@shzu.edu.cnReceivedJune12,2022;revisedAugust16,2022;publishedonlineSeptember15,2022.ProjectsupportedbytheNationalNaturalScienceFoundationofChina(Nos.21563025,22162022).国家自然科学基金(Nos.21563025,22162022)资助项目.Chin.J.Org.Chem.2023,43,195～201©2023ShanghaiInstituteofOrganicChemistry,ChineseAcademyofScienceshttp://sioc-journal.cn/195DOI:10.6023/cjoc202206017研究论文I2催化β-酮腈与1H-吡唑-5-胺的环化反应桑田贾帆何静李春天刘岩*刘平*(石河子大学化学化工学院化工绿色过程兵团重点实验室新疆石河子832003)摘要开发了一种碘催化的1H-吡唑-5-胺和β-酮基腈的环化反应,用来合成吡唑并[1,5-a]嘧啶.该方法提供了获得结构多样的吡唑并[1,5-a]嘧啶衍生物的有效途径,其产率可达到良好至优秀.该方法具有反应条件简单温和、底物范围广等优点,并可以克级规模放大反应.关键词I2催化;环化反应;吡唑并[1,5-a]嘧啶I2-CatalyzedCyclizationofβ-Ketonitrilewith1H-Pyrazol-5-amineSang,TianJia,FanHe,JingLi,ChuntianLiu,Yan*Liu,Ping*(KeyLaboratoryforGreenProcessingofChemicalEngineeringofXinjiangBingtuan,SchoolofChemistryandChemicalEngineering,ShiheziUniversity,Shihezi,Xinjiang832003)AbstractAnI2-catalyzedcyclizationreactionof1H-pyrazol-5-amineandβ-ketonitrileforthesynthesisofpyrazolo[1,5-a]pyrimidineswasdeveloped.Thismethodprovidesanefficientwaytoobtainstructurallydiversepyrazolo[1,5-a]pyrimidinederivativesingoodtoexcellentyields.Themethodhastheadvantagesofsimpleoperation,mildreactionconditionsandawiderangeofsubstrates.Itcanalsobescaledup.KeywordsI2-catalyzed;cyclizationreaction;pyrazolo[1,5-a]pyrimidines1IntroductionPyrazolo[1,5-a]pyrimidinesareanimportantclassofheterocycliccompoundsthathavebeenwidelyusedinmedicineandagrochemicals,[1]suchasthesleepingdrugsIndiplon[2]andZaleplon,[3]theanxiolyticdrugOcinaplon,[4]andthefungicidePyrazophos[5](Figure1).[6-7]Therefore,theconstructionofpyrazolo[1,5-a]pyrimidineshasattractedextensiveattentioninthefieldoforganicsynthesis.In2006,Barsyetal.[8]used5-amino-3-phenylpyrazoleandtri-p...
