L-脯氨酸催化一锅法合成4H-吡喃并[2,3-c]吡唑衍生物  被引量:2

L-proline catalyzed one-pot synthesis of 4H-pyrano[2,3-c]pyrazoles

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作  者:雷英杰[1] 丁玫[1] 姚庆佳 LEI Ying-jie;DING Mei;YAO Qing-jia(School of Chemistry&Chemical Engineering,Tianjin University of Technology,Tianjin 300384;Sphinx Scientific Laboratory Corporation,Tianjin 300457,China)

机构地区:[1]天津理工大学化学化工学院,天津300384 [2]天津市斯芬克司药物研发有限公司,天津300457

出  处:《化学研究与应用》2020年第6期1047-1052,共6页Chemical Research and Application

摘  要:以L-脯氨酸为绿色催化剂,3-甲基-5-吡唑酮(或1-苯基取代物)和芳醛及丙二腈为原料,就微波辅助的一锅法成环缩合反应进行研究。实验结果表明,乙醇/水为溶剂,催化剂用量10mol%,微波功率300W和80℃下反应10~15min,即可得到4H-吡喃并[2,3-c]吡唑类化合物(4a^4j),合成收率达85~94%。该方法具有产率高、反应时间短、操作简单等优点。A convenient procedure via one-pot cyclocondensation of 3-methyl-pyrazolidin-5-one or 3-methyl-1-phenyl-5-pyrozolene,aromatic aldehydes and malononitrile in the presence of L-proline in mixed solvent of ethanol and water under microwave irradiation was discussed.The results indicated that the green catalyst was efficient with the amount of 10mol%under irradiation at 300W with a temperature of 80℃for 10~15 min to afford 4 H-pyrano[2,3-c]pyrazole derivatives(4a^4j)with good yields of 85~94%respectively.The protocol proved to be efficient and clean in terms of high yields,low reaction times and ease of work-up.

关 键 词:4H-吡喃并[2 3-c]吡唑 L-脯氨酸 微波辐射 

分 类 号:O626.2[理学—有机化学]

 

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