Convenient synthesis of 1-phenyl-1,2-propanediamines. Preliminary pharmacological results.
A novel synthesis of (1R,2S)- and (1S,2S)-1-phenyl-1,2-propanediamines by highly regioselective and stereo-specific opening of chiral aziridines is reported. This method permits the synthesis of optically pure diastereomers. A hypothermic effect is observed after intracerebroventricular injection in rats.
Tytgat
D
D
Department of Pharmaceutical Organic Chemistry, Free University of Brussels, Belgium.
Gelbcke
M
M
Smith
D F
DF
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000138:chemical synthesis*; D003864:Depression, Chemical; D003959:Diamines / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D007276:Injections, Intraventricular; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003959:Diamines