DEPBT as Coupling Reagent To Avoid Racemization in a Solution-Phase Synthesis of a Kyotorphin Derivative

被引：7

作者：

Ramu, Vasanthakumar G. ^{[1
]}

Bardaji, Eduard ^{[1
]}

Heras, Montserrat ^{[1
]}

机构：

[1] Univ Girona, Dept Chem, Innovat Lab Organ Chem Proc & Prod LIPPSO, Girona 17071, Spain

来源：

SYNTHESIS-STUTTGART | 2014年 / 46卷 / 11期

关键词：

amide bond formation; coupling reagent; DEPBT; kyotorphin; racemization; REMARKABLE RESISTANCE; PEPTIDE-SYNTHESIS; DIPEPTIDE; BRAIN;

D O I：

10.1055/s-0033-1341068

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The synthesis of IbKTP-NH2 with reduction of racemization up to no detectable level has been achieved using 3-(diethoxyphosphoryloxy)-1,2,3-benzotriazin-4(3H)-one (DEPBT). Among all coupling systems tested, only DEPBT-mediated amide bond formation between N-alpha-acylated tyrosine and arginine without loss of optical purity.

引用

页码：1481 / 1486

页数：6

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