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- Title
Solvent-free synthesis and antiviral activity of chiral dialkyl 2-(substituted-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)methyl) malonate.
- Authors
Song Bai; Shan Liu; Yunying Zhu; Jiali Lu; Lina Ai; Jing Xue; Qin Wu
- Abstract
An efficient asymmetric synthesis of chiral ß-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.
- Subjects
MALONATES; AMINO acid derivatives; TOBACCO mosaic virus; ENANTIOSELECTIVE catalysis; PYRIDINE synthesis
- Publication
Journal of Chemical Research, 2018, Vol 42, Issue 8, p428
- ISSN
1747-5198
- Publication type
Article
- DOI
10.3184/174751918X15339142171145