| 摘要 |
Cpds. of formula (I) and their salts: - where R1 = Me or Et, R2 = C1-3 alkyl or allyl, R3 = H or Me, X1 = H, Cl, or CF3. - (I) have CNS sedative activity, as shown by their anticonvulsant effect in the anti-pentamethylene-tetrazole test (pharmacological data are given in the specification). - (II; R1 = R2 = Me, R3 = H, X1 = H) (9 g.), EtOOCCH2NH2.HCl (18 g.), piperidine (2 ml.), and pyridine (100 ml.) are stirred 30 hrs. at reflux, then evapd. to dryness under reduced pressure. - The residue is partitioned between CH2Cl2 (250 ml.) and H2O (100 ml.). The CH2Cl2 phase is separated, treated with active charcoal and Na2SO4, filtered and evapd. under reduced pressure (I; R1 = R2 = Me, R3 = X1 = H), m.p. 267 - 70 deg. (from EtOH). 2.5 g. of the base are dissolved in 15 ml. of ethanolic HCl.
|
