文献类型：期刊文献

英文题名：Solvent-free synthesis and antiviral activity of chiral dialkyl 2-(substituted-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)methyl) malonate

作者：Bai, Song Liu, Shan Zhu, Yunying Lu, Jiali Ai, Lina Xue, Jing Wu, Qin

第一作者：柏松

通信作者：Bai, S[1]

机构：[1]Guizhou Inst Technol, Sch Chem Engn, Guiyang 550003, Peoples R China;[2]Guiyang Municipal Publ Secur Bur, Drug Identificat Ctr, Guiyang 550081, Peoples R China;[3]Guizhou Univ Engn Sci, Bijie 551700, Peoples R China

第一机构：贵州理工学院化学工程学院

通信机构：corresponding author), Guizhou Inst Technol, Sch Chem Engn, Guiyang 550003, Peoples R China.|贵州理工学院化学工程学院;贵州理工学院;

年份：2018

卷号：42

期号：8

起止页码：428-433

外文期刊名：JOURNAL OF CHEMICAL RESEARCH

收录：;Scopus(收录号：2-s2.0-85052862964);WOS:【SCI-EXPANDED(收录号:WOS:000443731600009)】；

基金：We are grateful for financial support from the National Natural Science Foundation of China (Grant No. 21602039), the Natural Science Foundation of Guizhou Province (Grant No. Qian Ke He Ji Chu [2017] 1066), the Foundation of the Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University (Grant No. 2016GDGP0103), the Research Center for Microreaction Engineering of Guizhou Colleges and Universities (Grant No. Qian Jiao He KY Zi [2015] 339), the Academic Sprout Cultivation and Exploring Innovation Project of Guizhou Institute of Technology (Grant No. Qian Ke He Ping Tai Ren Cai [2017] 5789-06), the Science and Technology Research Projects of Guizhou Province (Grant No. Qian Ke He J Zi [2012] 2011). We would also like to thank LetPub (www.letpub.com) for providing linguistic assistance during the preparation of this manuscript.

语种：英文

外文关键词：solvent-free; asymmetric synthesis; beta-amino acid ester derivatives; tobacco mosaic virus

摘要：An efficient asymmetric synthesis of chiral beta-amino acid ester derivatives containing a 4-(pyridin-3-yl)pyrimidin-2-yl amine moiety was developed. This catalytic asymmetric Mannich reaction gave target products in high yields (95%) and excellent enantioselectivities (>99% ee) using a cinchona-based squaramide catalyst under solvent-free, one-pot conditions. Antiviral bioassays indicated that some of the chiral products exhibited higher antiviral activities against tobacco mosaic virus than the commercial compound ribavirin.