| 摘要 |
<p>Process for preparing cmpds. of general formula (I): (where R1 is 1-5C alkyl and R2 and R3 are same of different gps. of formula (II): where R4, R5 and R6 are same or different H, F, Cl, Br, 1-3C alkyl or alkoxy, -NO2 or -CF3, but no more than one of R4, R5 and R6 may be -NO2, -CF3, branched alkyl or alkoxy, and R1 is 2-5C alkyl if R2 and R3 are Ph) by oxidising cpds. having the general formula (III): (where either (1) p is H and q and r together denote a 2nd. bond, or (2) r is H and p and q together denote a 2nd. bond; R2' and R3' are the same as R2 and R3 except that neither R2' nor R3' contain an -NO2 gp. if p, q and r are as in (2)) in an inert organic solvent. (I) are tranquillisers-sedatives/hypnotics and are CNS-depressants (60-2000 mg/day in 2-4 doses, 15-100 mg. each). (I) where R2 and R3 denote and Rk4 is H, F, Cl or Br, are sleeping-drugs (120-2000 mg. at bed-time). (I) with unsubstd. Ph in positions 4 and 6 are antiinflammatory agents (120-2000 mg/day 2-4 times daily). 1-Me-4-Ph-6(3',4'-dimethoxy)phenyl-pyrimidine-2(1H)-one, 217-219 degrees C m.pt. (from CH2Cl2/Et2O) was obtd.</p> |
