Synthesis of Boc-Asp(OBzl)-β-Ala-Asp(OBzl)-N(OMe)Me as a Useful Precursor of Aspartyl Peptide Aldehyde Derivatives  

天冬氨酸肽醛衍生物前体Boc-Asp(OBzl)-β-Ala-Asp(OBzl)-N(OMe)Me的合成(英文)

作　　者：邹晓民[1] 赵宏[1] 傅翌秋[1] 张欣[1] 徐萍[1] 

机构地区：[1]北京大学药学院药物化学系,北京100083

出　　处：《Journal of Chinese Pharmaceutical Sciences》2003年第3期123-126,共4页中国药学（英文版）

基　　金：SupportedbytheNationalNaturalScienceFoundationofChina (2 0 2 72 0 04,20342003)andtheNationalMajorProgramforBasicResearchDevelopment(project973)fromtheMinistryofScienceandTechn ologyofChina (G19980 5 1114 )

摘　　要：Aim To synthesize the tripepide Weinreb amide Boc Asp(OBzl) β Ala Asp(OBzl) N(OMe)Me (7) as a useful precursor of aspartyl peptide aldehyde derivatives; Methods DCC, IBCF method was used for preparation of Weinreb amide; N hydroxysuccinimide activated ester was used in peptide synthesis; and Boc as N protecting group of amino acid. Results Boc Asp(OBzl) N(OMe)Me (3), Boc β Ala Asp(OBzl) N(OMe)Me (5), and Boc Asp(OBzl) β Ala Asp(OBzl) N(OMe)Me (7) were synthesized successfully. Conclusion An useful precursor of tripeptide aspartyl aldehydes was synthesized.目的　为了合成天冬氨酸三肽醛衍生物前体 ,Weinreb酰胺Boc Asp(OBzl) β Ala Asp (OBzl) N(OMe)Me。方法　采用DCC ,IBCF法合成Weinreb酰胺 ;N 羟基琥珀酰亚胺活化酯用于肽合成 ;Boc作为氨基酸的N 保护基。结果　成功合成了Boc Asp(OBzl) N(OMe)Me ( 3) ,Boc β Ala Asp(OBzl) N(OMe)Me ( 5 ) ,andBoc Asp(OBzl) β Ala Asp(OBzl) N(OMe)Me ( 7) 。

关 键 词：Weinreb amide aspartyl peptide aldehyde Boc protecting group activated ester 

分 类 号：R914[医药卫生—药物化学]