用N,N’-二环己基碳二亚胺(DCC)/1-羟基-苯并-三氮唑(HOBt)、1-乙基-(3-二甲基氨基丙基)碳酰二亚胺(EDC)/HOBt、2-乙氧基-1-乙氧碳酰基-1,2-二氢喹啉(EEDQ)、3-(二乙氧基磷酰基)-氧-1,2,3-苯并三嗪4(3H)-酮(DEPBT)4种常用缩合试剂合成了含N-Me二肽Boc-Leu—N—Me-Leu-OBzl,产率分别为73.5%~92.8%,65.2%~85.9%,38.9%,87.8%.比较发现反应物Boc-Leu-OH、H-N—Me-Leu-OBzl与缩合试剂DCC/HOBt的物质的量比在2.0:1.0:2.0时产率最高.利用此比例合成了3个立体异构体,产率较高.
Dipeptide Boc-Leu-N-Me-Leu-OBzl containing N-Me was synthesized with four different coupling reagents. After activated by coupling reagents such as DCC/HOBt, EDC/HOBt, EEDQ and DEPBT, the yield were 73.5% ~92. 8%, 65.2% -85.9% , 38.9%, 87.8%, respectively. The yield was higher than any of other coupling reagents when the molar ratio of Boc-Leu-OH/H-N-Me-Leu-OBzl/ DCC/HOBt was 2. 0: 1, 0: 2. 0. Three stereoisomers were gotten by coupling reagent DCC/HOBt with high yield when the molar ratio was 2.0: 1.0: 2. 0