(A) Cpds. of general formula (I) X=Cl or Br, R1=H or (1-3C) alkyl R2 and R3=H, alkyl opt. subst. by O-alkyl, CN, N(alkyl)2 or CO2 alkyl, alkenyl, cy

摘要

(A) Cpds. of general formula (I) X=Cl or Br, R1=H or (1-3C) alkyl R2 and R3=H, alkyl opt. subst. by O-alkyl, CN, N(alkyl)2 or CO2 alkyl, alkenyl, cycloalkyl, PhCH2, Ph, or adamantyl or opt. substd. by lower alkyl, Ph2CH- or by Ph opt. subst. by hal, Me, MeO, or NO2. (B) Salts of I. Analgesics, sedatives, anticonvulsants, and antitussives. LD50 ca. 300-600 mg/kg. 4-amino-3,5-dibromoacetophenone (29.5 g), N-methylethylamine HCl (12.5 g), paraformaldehyde (10 g), c HCl (2 ml) and EtOH (100 ml) were refluxed 64 hr., cooled, filtered, washed (Me2CO), and recryst. from MeOH Aq. giving I, HCl, m.p 220-222 deg.