Synthesis and Evaluation of a Series of 3, 4, 5??Trimethoxycinnamic Acid Derivatives as Potential Antinarcotic Agents

JC Jung, S Moon, D Min, WK Park…

Index: Jung, Jae-Chul; Moon, Sohyeon; Min, Dongguk; Park, Woo Kyu; Jung, Mankil; Oh, Seikwan Chemical Biology and Drug Design, 2013 , vol. 81, # 3 p. 389 - 398

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Abstract

A series of 3, 4, 5-trimethoxycinnamic acid derivatives was prepared and evaluated for antinarcotic effects on morphine dependence in mice and binding affinities on serotonergic receptors. The key synthetic strategies involve generation of ketones 6–7, esters 9–12 through condensation reaction, and amides 13–19 via coupling reaction using 1- hydroxybenzotriazole⁄ ethyl (dimethylaminopropryl) carbodiimide system in high yield. We ...