由LiN(SiMe)/CsF介导的吲哚啉-3-酮的一锅法合成。
One-Pot Synthesis of Indolin-3-ones Mediated by LiN(SiMe)/CsF.
作者信息
Ma Ruyuan, Gu Yuanyun, Wang Yan-En, Fei Rongbi, Xiong Dan, Mao Jianyou
机构信息
School of Chemistry and Molecular Engineering, Nanjing Tech University, 30 South Puzhu Road, Nanjing 211816, P. R. China.
College of Science, Hebei Agricultural University, Baoding 071000, P. R. China.
出版信息
Org Lett. 2024 Jun 21;26(24):5082-5086. doi: 10.1021/acs.orglett.4c01265. Epub 2024 Jun 7.
Indolin-3-ones are essential heterocycles with wide-ranging biological activities and medicinal values, and therefore, efficient approaches to their synthesis remain in demand. Herein, a novel and operationally simple method to generate indolin-3-ones is reported by using a tandem reaction of -methylbenzylamines and methyl 2-fluorobenzoates mediated by the LiN(SiMe) and CsF system (34 examples, 30-85% yields). The synthesis of C2-quaternary indolin-3-one further demonstrated the potential practicability of these tandem reactions.
吲哚-3-酮是一类具有广泛生物活性和药用价值的重要杂环化合物，因此，仍需要开发高效的合成方法。本文报道了一种新颖且操作简便的生成吲哚-3-酮的方法，该方法利用LiN(SiMe)和CsF体系介导的α-甲基苄胺与2-氟苯甲酸甲酯的串联反应（34个实例，产率30-85%）。C2-季碳吲哚-3-酮的合成进一步证明了这些串联反应的潜在实用性。
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