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Facile One-Pot Preparation of 5-Substituted 4-Iodo-1-tosylpyrazoles from N-Propargyl-N′-tosylhydrazines through Iodocyclization
Synthesis ( IF 2.2 ) Pub Date : 2022-03-28 , DOI: 10.1055/s-0041-1737395 Hideo Togo , Aya Saito , Kazuhiro Yoshida
中文翻译:
通过碘环化从 N-炔丙基-N'-甲苯磺酰肼轻松一锅法制备 5-取代的 4-Iodo-1-tosylpyrazoles
更新日期:2022-03-28
Synthesis ( IF 2.2 ) Pub Date : 2022-03-28 , DOI: 10.1055/s-0041-1737395 Hideo Togo , Aya Saito , Kazuhiro Yoshida
Treatment of N-propargyl-N′-tosylhydrazines with molecular iodine (I2) in the presence of NaHCO3 under warming conditions gave efficiently the corresponding 5-substituted 4-iodo-1-tosylpyrazoles in good to moderate yields. In addition, the same reaction in the presence of acetic acid generated the corresponding 5-aryl-4-iodopyrazoles in moderate yields. The reactions are simple and efficient transition-metal-free methods for the preparation of 5-substituted 4-iodopyrazole unit.
中文翻译:
通过碘环化从 N-炔丙基-N'-甲苯磺酰肼轻松一锅法制备 5-取代的 4-Iodo-1-tosylpyrazoles
在升温条件下,在 NaHCO 3存在下用分子碘 (I 2 )处理N-炔丙基-N'-甲苯磺酰基肼,以良好至中等的产率有效地产生相应的 5-取代的 4-碘-1-甲苯磺酰基吡唑。此外,在乙酸存在下的相同反应以中等收率产生相应的 5-aryl-4-iodopyrazoles。该反应是制备5-取代4-碘吡唑单元的简单有效的无过渡金属方法。