Convenient copper-mediated Chan–Lam coupling of 2-aminopyridine: facile synthesis of N-arylpyridin-2-amines
摘要:
A new and practical process for the synthesis of N-arylpyridin-2-amine derivatives has been developed. Under the assistance of copper, the desired products were produced from commercially available 2-aminopyridine and aryl boronic acids in moderate to good yields with good functional group tolerance. (C) 2015 Elsevier Ltd. All rights reserved.
autoclave‐free protocol for the synthesis of 11H‐pyrido[2,1‐b]quinazolin‐11‐ones has been developed. Quinazolinones, which are omnipresent motif in many pharmaceuticals and agrochemicals, were prepared in good yields by CH bond activation and annulation using DMF as the CO surrogate. A 13CO‐labelled DMF control experiment demonstrated that CO gas was released from the carbonyl of DMF with acid as
为11的合成一种新型的钯催化CO-气体和无高压釜协议ħ -吡啶并[2,1- b ]喹唑啉-11-那些已经研制成功。喹唑啉酮是许多药物和农用化学品中无处不在的基序,它是通过CH键活化和使用DMF作为CO替代物进行环化而制备的,产率很高。一项13 CO标记的DMF对照实验表明,以酸为促进剂从DMF的羰基中释放出CO气体。的动力学同位素效应(KIE)值指示,在C ħ活化步骤可以不是在速率决定步骤有关。该方法操作简单,显示了广泛的底物范围,具有良好至极好的产率。
Pd/C-catalyzed carbonylative C–H activation with DMF as the CO source
作者:Jianbin Chen、Kishore Natte、Xiao-Feng Wu
DOI:10.1016/j.tetlet.2015.09.142
日期:2015.11
An interesting Pd/C-catalyzed carbonylative cyclization of N-arylpyridin-2-amine derivatives via C-H activation has been developed. With DMF as the CO source, the desired quinazolinones were formed in moderate to good yields with good functional group tolerance. (C) 2015 Elsevier Ltd. All rights reserved.