Franco Manfre

Enantiospecific synthesis and absolute configuration of (+)-RP 66803 a new non-peptide CCK antagonist

Abstract Pyrrolidine derivatives have been identified as a new class of non-peptide CCK antagonists. Enantiomers of RP 66803 , a representative compound of this chemical family were previously prepared by chiral chromatography of the racemate. In order to determine the absolute configuration of each one, we report herein an enantiospecific synthesis leading to the (+)-isomer using anodic methoxylation as key step.

Convenient Syntheses of Racemic 2-(3-Nitrophenyl)propanoic Acid and 2-(3-Aminophenyl)propanoic Acid

Abstract 2-(4-Chlorophenyl)propanoic acid 1 is transformed to 2-(4-chloro-3-nitrophenyl) propanoic acid 2 (94% yield). Acid 2 can be converted to 2-(3-nitrophenyl)propanoic acid 3 (70% yield) or to 2-(3-aminophenyl) propanoic acid 4 (80% yield).