Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210028, Jiangsu, China.
Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210028, Jiangsu, China.
J Org Chem. 2021 Nov 5;86(21):15640-15647. doi: 10.1021/acs.joc.1c02175. Epub 2021 Oct 21.
A one-pot, two-step protocol for the synthesis of libraries of remarkable functionalized sulfone analogues of 9b,10,10a,10b-tetrahydro-1-cyclopropa[][1,4]thiazino[4,3-]quinolines is described. A class of various functionalized molecular skeletons was obtained by cyclopropanation of quinolinium zwitterionic thiolates. The reaction pathway involves the formation of a [2 + 1] cycloaddition intermediate followed by a [5 + 1] cycloaddition.
本文描述了一种一锅两步法合成 9b,10,10a,10b-四氢-1-环丙基[][1,4]噻嗪并[4,3-]喹啉的磺酸酯类似物文库的方法。通过喹啉翁硫代内盐的环丙烷化反应得到了一系列各种功能化的分子骨架。该反应途径涉及[2 + 1]环加成中间体的形成,然后是[5 + 1]环加成。