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钯(II)催化通过 C(sp)-H 活化 -不饱和 -乙酰腙与乙烯基叠氮化物合成脂环[ ]稠合吡啶。

Pd(II)-Catalyzed Synthesis of Alicyclic[]-Fused Pyridines via C(sp)-H Activation of -Unsaturated -Acetyl Hydrazones with Vinyl Azides.

机构信息

Key Laboratory of Functional Molecular Engineering of Guang-dong Province, School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou 510640, China.

State Key Laboratory of Anti-Infective Drug Development (No. 2015DQ780357), Sunshine Lake PharmaCompany, Ltd., Dongguan 523871, China.

出版信息

J Org Chem. 2022 Jan 7;87(1):159-171. doi: 10.1021/acs.joc.1c02086. Epub 2021 Dec 21.

Abstract

A new synthetic protocol for alicyclic[]-fused pyridines with complete regioselectivity from unsaturated -acetyl hydrazones and vinyl azides via Pd(II)-catalyzed C-H activation/cyclization/aromatization strategy has been described. A series of five- to eight-membered alicyclic[]-fused pyridines were prepared in a one-step manner with wide substrate scope and good functional group tolerance.

摘要

已描述了一种新的通过 Pd(II)催化的 C-H 活化/环化/芳构化策略,从不饱和 -乙酰腙和乙烯基叠氮化物出发,以完全区域选择性合成脂环[ ]-稠合吡啶的合成方案。通过一步法制备了一系列五至八元脂环[ ]-稠合吡啶,具有广泛的底物范围和良好的官能团耐受性。

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