N-甲基二肽MeVal-MePhe-O^tBu的合成研究  

Synthesis of N-Methyldipeptide MeVal-MePhe-O^tBu

作　　者：王晓季[1] 陈立功[1] 李阳[1] 

机构地区：[1]天津大学药物科学与技术学院,天津300072

出　　处：《精细化工》2004年第6期434-438,共5页Fine Chemicals

摘　　要：以邻硝基苯磺酰氯对L 缬氨酸和L 苯丙氨酸的氨基进行活化,经甲基化、偶合、脱除等7步反应,合成了对人体肿瘤细胞KB和LoVo具有中等细胞毒性的天然环酯肽Obyanamide[1]中具有较大空间位阻的N 甲基二肽结构片段MeVal MePhe OtBu,总收率达48 2%。Hindered N-methyldipeptide(MeVal-MePhe-O^tBu),the segment of a novel cyclic depsipeptide Obyanamide which exhibits moderate cytotoxicity against KB and LoVo cells,was synthesized from L-valine and L-phenylalanine in overall yield of 48.2%.This synthesis was accomplished in seven steps from N-Ns-(L)-Val-O^tBu and N-Ns-(L)-Phe-O^tBu which were activated with 2-nitrobenzenesulfonyl chloride.

关 键 词：邻硝基苯磺酰氯 L-缬氮酸 L-苯丙氮酸 N-甲基二肽 

分 类 号：O621.3[理学—有机化学]