X. Jing
2004
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Journal
Chinese Journal of Pharmaceuticals
Abstract
S)-(-)-N-(1-Allylpyrrolidin-2-ylmethyl)-5-(3-hydroxypropyl)-2,3-dimethoxybenzamide, a inter-mediate of 18F-fallypride was synthesized from 2-hydroxy-3-methoxybenzoic acid methyl ester(5) by allylation, Claisenrearrangement, methylation, hydroboration and hydrolysis to afford 2,3-dimethoxy-5-(3-hydroxypropyl)benzoic acid, andthen followed by amidation with (S)-(-)-2-aminomethyl-N-allylpyrrolidine which prepared from 2-carbamylpyrrolidineby alkylation and reduction. The overall yield was 51.9%(based on 5).