| 摘要 |
<p>New p-acetyl-phenethylamines are of formula (I) (in the form of the racemates, pure stereoisomers and possible diastereomer-pairs) and their acid addition salts:- (where R1, R2 = H or Me R3 = C1-3 alkyl R4 = H, C1-3 alkyl subst. by an OH group or Cl atom, theophyllin-7-ylethyl, carbalkoxy or carbobenzoxy) Useful as appetite-inhibitors with low motor-stimulant activity. Thus, with (I; R1=R2=R4=H, R3=Me) (which has greater appetite-inhibiting activity than diethylpropion), the ratio of the feeding-inhibiting ED50 to the motor-stimulant ED5000 (both in mg/kg s.c. in rats) is ca. 21:1, while the same ratio for diethylpropion is less than 1:1. Prepared as follows:- + CH3CO-X friedel-Crafts (I) (X = Cl, Br or CH3CO2-).</p> |
