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四种缩合试剂对含N-Me二肽的合成 被引量：2

Four coupling reagents for synthesis of N-methyldipeptide
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摘要 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
作者 刁建忠 许文杰 廖小建 徐石海
机构地区 暨南大学化学系
出处 《暨南大学学报（自然科学与医学版）》 CAS CSCD 北大核心 2009年第3期298-301,共4页 Journal of Jinan University(Natural Science & Medicine Edition)
基金 国家863基金项目(2006AA09Z408) 国家自然科学基金项目(20772048) 广东省自然科学基金项目(06025194 2005A30503001 2006Z3-E4041)
关键词 缩合试剂 亮氨酸 肽 coupling reagent leucine peptide
分类号 O62 [理学—有机化学]
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参考文献17

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共引文献24

同被引文献30

  • 1沈鸿雁,刘镇宁,晏皖琳,叶蕴华,田桂玲.咪唑基引起缩合试剂3-(二乙氧基磷酰基)-氧-1,2,3-苯并三嗪-4(3H)-酮(DEPBT)的副反应[J].高等学校化学学报,2006,27(7):1289-1291. 被引量：1
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引证文献2

二级引证文献3

暨南大学学报（自然科学与医学版）
2009年 第3期

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