Chu C K, Jin Y H, Baker R O, Huggins J
Department of Pharmaceutical and Biomedical Science, College of Pharmacy, The University of Georgia, Athens 30602, USA.
Bioorg Med Chem Lett. 2003 Jan 6;13(1):9-12. doi: 10.1016/s0960-894x(02)00841-7.
An improved method for the synthesis of enantiomerically pure D-cyclopentenyl nucleosides has been accomplished and their antiviral activity against orthopox viruses have been evaluated. The key intermediate, L-cyclopent-2-enone 13 was prepared from D-ribose using a ring closing metathesis reaction in eight steps. Among the synthesized nucleosides, the adenine 2 (Neplanocin A), cytosine 14, and 5-F-cytosine 15 analogues exhibited potent anti-orthopox virus activity, including smallpox virus.
已经完成了一种合成对映体纯的D-环戊烯基核苷的改进方法,并评估了它们对正痘病毒的抗病毒活性。关键中间体L-环戊-2-烯酮13由D-核糖通过闭环复分解反应分八步制备。在合成的核苷中,腺嘌呤2(奈拉滨)、胞嘧啶14和5-氟胞嘧啶15类似物表现出强大的抗正痘病毒活性,包括天花病毒。