3-哌啶甲酸及其衍生物的合成与应用研究进展有机化学.pdfVIP

2009 年第 29 卷 有 机 化 学 Vol. 29, 2009 第 7 期, 1068～1081 Chinese Journal of Organic Chemistry No. 7, 1068～1081 ·综述与进展· 3-哌啶甲酸及其衍生物的合成与应用研究进展 李运波 唐凤翔* 孟 春 郭养浩 (福州大学药物生物技术与工程研究所 福州 350108) 摘要 3-哌啶甲酸及其衍生物是重要的药物中间 , 具有很高的生物活性. 综述了 3-哌啶甲酸及其羧基酯化、不饱和、 不同位置取代与多取代衍生物的合成方法, 并对 3-哌啶甲酸及其衍生物在合成 γ-氨基丁酸(GABA)摄入抑制剂、抗肿瘤 药、生长激素促分泌素、消炎药物、心血管药物、促智药物、抗流感病毒、骨疾病等药物中的应用进行了概述. 关键词 3-哌啶甲酸; 3-哌啶甲酸衍生物; 药物中间 Progress in the Synthesis and Application of Nipecotic Acid and Its Derivatives Li, Yunbo Tang, Fengxiang* Meng, Chun Guo, Yanghao (Institute of Pharmaceutical Biotechnology and Engineering, Fuzhou University, Fuzhou 350108) Abstract Nipecotic acid and its derivatives, which have high bioactivity, are significant pharmaceutical intermediates. In this review, the synthetic methods of nipecotic acid and its derivatives are summarized. The application of nipecotic acid and its derivatives to synthesizing drugs for γ-aminobutyric acid (GABA) uptake inhibition, cancer chemotherapy, growth hormone secretion, anti-inflammation, cardiovascular dis- ease, Alzheimer’s disease, nootropics, anti-flu virus and bone disease is presented as well. Keywords nipecotic acid; nipecotic acid derivative; pharmaceutical intermediate 3-哌啶甲酸作为一种含有刚性哌啶环的非蛋白β- 氨 水溶液中加压氢化烟酸合成了 3- 哌啶甲酸, 收率为 基酸, 显示了较好的神经递质 γ-氨基丁酸(GABA)转运 88.57%; Valsborg 等[4]采用同样的催化剂和碱性介质经 蛋白抑制活性, 与 2-哌啶甲酸、4-哌啶甲酸同为合成多 长时间常压加氢制备 3-哌啶甲酸, 收率为 98%, 但铑在 种手性药物和生物活性