Abstract

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

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