Journal
SYNLETT
Volume 29, Issue 14, Pages 1921-1925Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0037-1609910
Keywords
one-pot; solvent-free; chiral -amino ester derivatives; Mannich reaction; antiviral bioactivity
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Funding
- National Natural Science Foundation of China [21602039]
- Natural Science Foundation of Guizhou Province, China [Qian Ke He Ji Chu[2017]1066]
- Opening Foundation of the Key Laboratory of Green Pesticide and Agricultural Bioengineering
- Ministry of Education, Guizhou University [2016GDGP0103]
- Research Center for Microreaction Engineering of Guizhou Colleges and Universities [Qian Jiao He KY Zi[2015]339]
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A series of both enantiomers of chiral -amino acid ester derivatives containing a 4-(piperidin-1-yl)pyrimidine moiety was prepared in high yield and excellent enantioselectivity excess (up to >99% enantiomeric excess) using a chiral cinchona alkaloid thiourea catalyst under one-pot solvent-free conditions. Antiviral bioassay experimental results showed that some of the chiral products exhibited higher antiviral activities against tobacco mosaic virus (TMV) in vivo than the commercial antiviral agent ningnanmycin.
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