N-(3-甲基-1-吡咯烷基)-1-丁酮基-苯丙酰胺的合成研究  

Study on the Synthesis of N-(3-methyl-1-pyrrolidinyl)-1-butan-oxo-benzenepropanamide

作　　者：陶李明[1,2] 刘文奇[1] 胡玉龙[3] 周芸[1] 伍跃东[1] 

机构地区：[1]湘南学院化学与生命科学系,郴州市423000 [2]湖南师范大学化学化工学院,长沙市410081 [3]湘南学院基础医学部,郴州市423000

出　　处：《中国药房》2010年第9期802-803,共2页China Pharmacy

基　　金：湖南省自然科学基金资助项目(08JJ3018);湖南省教育厅资助项目(08C828);湘南学院资助项目(2007Y009)

摘　　要：目的:合成心血管疾病新治疗靶点小分子白介素1受体/髓样分化蛋白88-TIR(Toll/IL-1receptor)(IL-1R/MyD88-TIR)拟似物N-(3-甲基-1-吡咯烷基)-1-丁酮基-苯丙酰胺。方法:以N-叔丁氧羰基-L-缬氨酸羟基琥珀酰亚胺酯为原料,先合成3-甲基-2-叔丁氧羰氨基-1-吡咯烷基-1-丁酮,再合成N-(3-甲基-1-吡咯烷基)-1-丁酮基-苯丙酰胺,产物结构经核磁共振(NMR)和质谱(MS)确证。结果:通过2步反应合成了N-(3-甲基-1-吡咯烷基)-1-丁酮基-苯丙酰胺,反应总收率为81.1%,产物结构经NMR和MS证实为目标化合物。结论:该反应条件温和,操作方便,收率较高。OBJECTIVE： To synthesize analogue of IL-1RJMyD88-TIR with low molecular weight, i.e. N-（3-methyl-l-pyrrolidinyl） - 1-butan-oxo-benzenepropanamide. METHODS： Firstly, 3-methyl-lpyrrolidinyl- 1-butanone was synthesized using N-tertiary-butoxycarbonyl-L-valine hydroxysuccinimide eater as the initial material. Secondly, N-（3-methy1-1-pyrrolidiny1）-1-butan-oxo-benzenepropanamide was synthesized. The structure of product was detected by NMR and MS spectrum. RESULTS： N-（3-methyl-1-pyrrolidiny1）-1-butan-oxo-benzenepropanamide was synthesized successfully by two steps. The yield of the production was up to 81.1%. The structure of product detected by NMR an MS spectrum was affirmed as the target compound. CONCLUSION： The reaction was readily performed with good yield under mild conditions and convenient operations.

关 键 词：N-(3-甲基-1-吡咯烷基)-丁酮基-苯丙酰胺 合成 收率 

分 类 号：R914.5[医药卫生—药物化学]