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Synthesis 2014; 46(11): 1481-1486
DOI: 10.1055/s-0033-1341068
DOI: 10.1055/s-0033-1341068
paper
DEPBT as Coupling Reagent To Avoid Racemization in a Solution-Phase Synthesis of a Kyotorphin Derivative
Further Information
Publication History
Received: 14 February 2014
Accepted after revision: 06 March 2014
Publication Date:
02 April 2014 (online)
Abstract
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 Nα-acylated tyrosine and arginine without loss of optical purity.
Supporting Information
- for this article is available online at http://www.thieme-connect.com/ejournals/toc/synthesis.
- Supporting Information
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