| 摘要 |
(A) Compds. of general formula (I): R = OH or NR2R3 and R1, R2 and R3 = H, Me, or Et. (B) Acid addn. salts of (I). Anti-virals, esp. active v.s. influenza-A and with low toxicity and CNS activity. Dose 50 - 500 mg./d. (a) Adamantanone (2.5 g.) was added to Me2SOCH2 (17 m.mol.) in Me2SO (18 ml.), at 20 deg., stirred 20 hrs. at 20 deg., 1 hr. at 50 deg., poured into H2O (45 ml.), and extd. with Et2O. The Et2O was washed, dried, and evapd., giving the oxiran (2.45 g.), m.p. 178 - 181 deg. (b) This (1 g.), NaNH2 (1.2 g.), and 1. NH3 (20 ml), were heated 2 days at 80 deg. in a sealed tube, cooled to -70 deg., openend, and evapd. The residue was dissolved in PhH, (20 ml.), filtered, evapd., treated with HCl-Et2O, and recryst. from Et2O-EtOH, giving I. HCl, m.p. 290 - 292 deg. |
