| 摘要 |
<p>PURPOSE:To obtain the subject new compound having excellent antiviral activity, low in cytotoxicity, resistant to adenosine deaminase, useful as a highly safe antiviral agent. CONSTITUTION:A compound of formula I (A is CH or N), e.g. (2S,3S,4R)-2,3- isopropylideneoxy-4-hydroxy-4-ethoxycarbonylmethyl-5-cyclopentene. The compound of formula I can be obtained by reaction of a cyclopentene derivative of formula II (R1-R3 are each protecting group for OH; X is electron-attractive eliminable group) with (B) an adenine derivative of formula III (R4 is H or amino-protecting group) in an inert solvent (e.g. DMF) at room temperature to elevated temperatures. The compound of formula I is highly large in chemotherapeutic index defined as the ratio of minimum cytotoxic concentration to viral proliferation-inhibitory concentration and also large in the difference between the concentration giving antiviral activity and that giving cytotoxicity, thus being a safe medicine.</p> |
