两个C2轴对称环十肽的合成  

Synthesis of Two C2 Symmetrical Cyclic Decapeptide

作　　者：陈建维[1] 白德发[1] 钟生辉[1] 曲桐[1] 徐石海[1] 

机构地区：[1]暨南大学生命科学技术学院化学系,广东广州510632

出　　处：《精细化工》2016年第2期162-167,194,共7页Fine Chemicals

基　　金：国家自然科学基金(21172094;41376155;21372100;U1301131);广州市科技项目(2013000000163);国家高技术研究发展计划(863计划)(2013AA092902)~~

摘　　要：以亮氨酸和苯丙氨酸为原料,通过氨基酸的保护以及脱保护、氨基酸的甲基化和耦合,最后以O-苯并三氮唑-N,N,N'N'-四甲基脲四氟硼酸酯(TBTU)/2-(7-偶氮苯并三氮唑)-N,N,N',N'-四甲基脲六氟磷酸酯(HATU)/3-(二乙氧基磷酰氧基)-1,2,3-苯并三嗪-4-酮(DEPBT)为环合试剂,合成2个C2轴对称环十肽化合物Q10-1与Q10-2,最后环合收率分别为31.6%和39%。通过HPLC进行分离纯化,经HPLC检测产物纯度均在98%以上,通过1HNMR,13CNMR和ESI-MS对两个化合物进行表征。With leucine and phenylalanine as raw materials,synthesized two C2 symmetrical cyclic decapeptide compounds Q10- 1 and Q10- 2 in assistance of protection and deprotection of amino acids,the amino acid methylation and coupling,and TBTU / HATU / DEPBT as cyclization reagents. The cyclization yield reached 31. 6% and 39%. The products were isolated and purified by HPLC,which the purity of product was up to 98% detected by HPLC. The compound structures were characterized by means of1 HNMR,13CNMR and ESI-MS.

关 键 词：海洋环肽 环十肽 表征 医药原料 

分 类 号：O629.725[理学—有机化学]