| abstract |
PURPOSE: To obtain a new compound having excellent anti-viral, paticularly anti-retroviral, activity, and useful for remedy and prevention against HTLV I or II infectious disease, for example, AIDS. n CONSTITUTION: This compound of the formula I and its salts, e.g. 1{(3R,4 S)-4-[(tert-butoxycarbonyl)amino]-5-cyclo-hexyl-3-hydroxypentanoyl}-(2R, S)-2-(pyrrolidinyl)-phosphonic acid diethylester is obtained, for example, by allowing the compound of the formula III to react with the compound denoted by the formula W-X (X is halogen, preferably Cl) in an inactive solvent in the presence of a base. In the formula I, W is H, amino-protecting group, etc.; A, B, D are each direct bond, the formula II ((x) is 1 or 2), etc.; R 1 is ≤10C chain alkyl, 6-10C aryl, etc.; (n) is 1 or 2; R 2 , R 2 ' are each hydroxyl, ≤8C alkoxy; E is CH 2 , CF 2 , etc. n COPYRIGHT: (C)1992,JPO |