| 摘要 |
<p>PURPOSE: To obtain an antiviral agent having potent antiviral, action, thus effective for various viral diseases such as herpes virus infectious diseased and AIDS, containing, as active ingredient, a cyclobutane derivative having specific structure. CONSTITUTION: This antiviral agent contains as active ingredient a (1R,2R,3S) cyclobutane derivative of formula I (B is a purine base; R<4> is H or a protecting group) e.g. 9-[(1R,2R,3S)-2,3-bis(hydroxymethyl)cyclobutan-1-yll-adenine}. The compound of formula I is obtained, for example, by reaction between a compound of formula II (X is an eliminable group) and a purine base such as adenine, guanine or 2-aminopurine. It is preferable that the above reaction be carried out at room temperature to 170 deg.C in a solvent such as DMF using 1-5 equivalents of the purine base per equivalent of the compound of formula II. The compound of formula I can be orally, intravenously or percutaneously administered, its dose being normally 0.1-500mg/kg b.w. a day.</p> |
