Artemisinin Research Center & The First Affiliated Hospital, Guangzhou University of Chinese Medicine, 12 Jichang Road, Guangzhou 510405, China.
Research Centre for Integrative Medicine, School of Basic Medical Science, Guangzhou University of Chinese Medicine, Guangzhou 510006, China.
J Org Chem. 2022 Jun 3;87(11):7480-7486. doi: 10.1021/acs.joc.2c00219. Epub 2022 May 12.
A convergent access to substituted 2-iminoimidazolidines from aromatic amines and -propargyl -methylthiourea is developed via Ag(I)-mediated cascade guanylation-cyclization reactions. This method features high regioselectivity, excellent efficiency, and mild reaction conditions. Subsequent deprotection of the Boc (-butyloxycarbonyl) group under acidic conditions provides expedient access to aryl 2-aminoimidazole derivatives in a convenient manner.
一种从芳基胺和 -炔丙基 -甲基硫脲出发的取代 2-亚氨基咪唑烷的收敛性合成方法通过 Ag(I)-介导的级联鸟苷化-环化反应得到。该方法具有高区域选择性、高效率和温和的反应条件。随后在酸性条件下脱除 Boc（-叔丁氧羰基）保护基，以方便的方式提供了方便的芳基 2-氨基咪唑衍生物。
