O-N型竞争smiles重排反应研究

O-N-type Competition Smiles Rearrangement

本研究是O-N型竞争smiles重排反应的首次发现和报道。通过对多种底物和多种条件的筛选,发现以2-甲基-5,7-二氟-8-羟基喹啉为底物,在Cs2CO3\Na H\NMP\DMPU\125℃条件下,反应按照竞争smiles重排反应路径进行,产率可达到83%。本论文的研究将给芳香环并恶嗪类药物中间体和精细化学品的合成,以及芳香酚类化合物到芳香胺类化合物的转化提供实验依据和理论指导。

This is O-N-type smiles rearrangement was first discovered and reported. Through a variety of substrates and screening of a variety of conditions, and we found that 2-methyl-5,7-difluoro-8-hydroxy quinoline as a substrate, at Cs2 CO3／Na H／NMP／DMPU／125 ℃ condition the reaction according to competition smiles rearrangement reaction path with a yield of up to 83 %. This paper will study the synthesis of the aromatic ring and dioxazine drug intermediates and fine chemicals, as well as the conversion of aromatic phenolic compound to aromatic amines provide experimental evidence and theoretical guidance.