Okunrobo Lucky O, Usifoh Cyril O, Scriba Gerhard K E
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Benin, Benin City, Nigeria.
Acta Pol Pharm. 2006 Jan-Feb;63(1):25-31.
The ring opening of some phthalimide derivatives with sodium borohydride in methanol/water (6:1) afforded the corresponding 2-hydroxymethylbenzamides irrespective of the substituents. The most active members of the series evaluated for anti-inflammatory and analgesic activities were 2-hydroxymethyl-N-[4-(2-methoxyphenyl)-piperazin-1-yl]-ethylbenzamide (3d) and 2-hydroxymethyl-N-[4-(2-methoxyphenyl)-piperazin-1-yl]-propylbenzamide (3e), respectively.
一些邻苯二甲酰亚胺衍生物在甲醇/水（6:1）中与硼氢化钠发生开环反应，无论取代基如何，均生成相应的2-羟甲基苯甲酰胺。该系列中经抗炎和镇痛活性评估的最具活性的成员分别是2-羟甲基-N-[4-(2-甲氧基苯基)-哌嗪-1-基]-乙基苯甲酰胺（3d）和2-羟甲基-N-[4-(2-甲氧基苯基)-哌嗪-1-基]-丙基苯甲酰胺（3e）。
