| 摘要 |
1391803 lmidazo[1,2-a]pryimidines BOEHRINGER INGELHEIM GmbH 7 July 1972 [8 July 1971] 32005/72 Heading C2C The invention comprises compounds of formula and their acid addition salts, wherein R 1 is Ph or PhCH 2 , possibly substituted by 1-3 of Me, Et, CF 3 , CN, MeO, F, C1 or Br, and A is -CR 2 = CR 3 -CO-, where at least one of R 2 , R 3 is -(CH 2 ) n NR<SP>1</SP>R<SP>11</SP>, n is 0-3 and NR<SP>1</SP>R<SP>11</SP> is alkylamino, dialkylamino, piperidino, piperazino, morpholino or pyrrolidino, and when R 2 or R 3 is not the said group, it is Me or Et, In examples, these compounds are prepared by reacting a 2-R 1 NH-2-imidazoline with a compound of formula Y-CR 2 = CR 3 -COX, X and Y each being a nucleophilic atom or group; the use of a polar protic solvent favours formation of the 5- oxo compound, and an aprotic solvent, the 7-oxo compound. Therapeutic compositions for oral, parenteral or rectal administration comprise compounds of the above formula, which are CNS regulators and in particular show hypotensive activity, possibly accompanied by an analgesic or sedative effect, or an inhibiting effect on gastric secretion. |
