Abstract

Synthesis of a new structural class of phenylalanine derivatives is described. Azidonation of Boc-L-Phe(4-I)-OMe via copper-ligand catalysis with sodium azide under microwave irradiation followed by regioselective copper-catalyzed azide-terminal alkyne cycloaddition provided new 4-(1,2,3-triazol-1-yl)-L-Phe derivatives. The developed protocol was also successfully employed to synthesize a late-stage modified Phe containing peptide.

中文翻译：

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4-(1,2,3-triazol-1-yl)-L-苯丙氨酸的合成

摘要

描述了一种新结构类别的苯丙氨酸衍生物的合成。Boc-L-Phe(4-I)-OMe 在微波辐射下通过铜配体催化与叠氮化钠的叠氮化反应，然后区域选择性铜催化叠氮化物末端炔烃环加成反应提供了新的 4-(1,2,3-triazol-1 -yl)-L-Phe 衍生物。所开发的方案也成功地用于合成后期修饰的含有 Phe 的肽。