By using a chiral cinchona alkaloid-squaramide catalyst, a series of both enantiomers of novel amino-pyrimidine derivatives can be obtained in an enantioselective three-component one-pot Mannich reaction with high yields and excellent enantioselectivities. In addition, these chiral derivatives were found to exhibit higher antiviral activities against tobacco mosaic virus (TMV) in vivo than the commercial agent ningnanmycin. In particular, chiral compounds (R)-4b and (R)-4e showed excellent antiviral activity against TMV at a concentration of 500 μg/mL, with a curative activity of 56.8% and 55.2%, respectively, a protection activity of 69.1% and 67.1%, respectively, and an inactivation activity of 91.5% and 94.3%, respectively. These values are superior to those of the agent ningnanmycin (which has curative, protective, and inactivation activities of 52.9%, 62.8%, and 90.4%, respectively). The antiviral mechanisms and enhanced antiviral activities of these chiral derivatives are interesting subjects for future investigation.

通过使用手性金鸡纳生物碱-方酸酰胺催化剂，可以在对映选择性三组分单锅曼尼希反应中以高收率和优异的对映选择性获得一系列新颖的氨基-嘧啶衍生物的两种对映体。此外，发现这些手性衍生物在体内对烟草花叶病毒（TMV）的抗病毒活性高于商业试剂宁南霉素。特别是手性化合物（R）-4b和（R）-4e在500μg/ mL的浓度下对TMV表现出优异的抗病毒活性，分别具有56.8％和55.2％的治愈活性，69.1％和67.1％的保护活性以及91.5％和94.3％的失活活性， 分别。这些值优于宁南霉素（其治愈，保护和灭活活性分别为52.9％，62.8％和90.4％）的值。这些手性衍生物的抗病毒机制和增强的抗病毒活性是未来研究的有趣课题。