Synthesis of protected aminoalkyl sulfinyl dilactones from α-amino acids  

保护的氨烷基化亚磺酰双内酯的合成(英文)

作　　者：付刚[1] 邹晓民[1] 傅翌秋[1] 牟科[1] 马超[1] 吕扬[1] 徐萍[1] 

机构地区：[1]北京大学药学院天然药物及仿生药物国家重点实验室,北京100083

出　　处：《Journal of Chinese Pharmaceutical Sciences》2007年第2期119-124,共6页中国药学（英文版）

基　　金：National Natural Science Foundation of China(20572006);985 Program,Ministry of Education of China

摘　　要：Aim To synthesize protected aminoalkyl sulfinyl dilactones which were useful as the synthetic intermediates or the Cterminal pharmacophores of potential peptidomimetic proteasome inhibitors. Methods Organic reactions such as reduction, oxidation, olcfmation, and dihydroxylation were used. Results A convenient synthetic procedure to afford a series of aminoalkyl sulfinyl.dilactones was presented, which would be useful in the synthesis of five- or six-member sulfmyl dilactones. Conclusion Four aminoalkyl sulfmyl dilactones connecting different α-amino acids were synthesized.目的合成了带有保护基的氨基烷基亚磺酰双内酯,此类化合物是一种有用的化学反应中间体,并且有可能作为蛋白酶体抑制剂的药效团。方法综合使用多种有机合成反应,包括还原反应、氧化反应、Wittig烯化反应、氧化成邻二醇的反应等。结果探索出一种合成保护的氨烷基化亚磺酰双内酯化合物的方便方法,此方法也适用于合成其他取代基的五元或六元环亚磺酰双内酯。结论从四种不同的带有保护基的氨基酸合成了四个带有保护基的氨烷基亚磺酰双内酯。

关 键 词：Proteasome inhibitors Protected aminoalkyl sulfmyl dilactone  Synthesis 

分 类 号：R914[医药卫生—药物化学]