School of Chemistry, The Sackler Faculty of Exact Sciences, Tel Aviv University, Tel Aviv, 69978, Israel.
Blavatnik Center for Drug Discovery, Tel Aviv University, Tel Aviv, 69978, Israel.
Angew Chem Int Ed Engl. 2022 Jul 18;61(29):e202205368. doi: 10.1002/anie.202205368. Epub 2022 Jun 2.
LPt F(Aryl) complexes bearing a bulky bidentate 2-[bis(adamant-1-yl)phosphino]phenoxide ligand (L) demonstrate excellent reactivity and selectivity in the arylation of X-H (X=S, N) bonds of amino acid residues in unprotected peptides under mild, including aqueous, conditions. Stepwise addition of these complexes allowed a convenient one-pot introduction of different aromatic groups in the X-H bonds of Cys and N terminus. Pt reagents can also be used to further arylate N-H bonds in Lys and Trp providing access to peptides bearing multiple aromatic groups.
带有大位阻双齿 2-[双(金刚烷-1-基)膦氧基]苯氧配体 (L) 的 LPt F(芳基) 配合物在温和条件下，包括水相条件下，展示出在未保护的肽中氨基酸残基的 X-H（X=S，N）键的芳基化反应中具有优异的反应性和选择性。这些配合物的逐步添加允许在 Cys 和 N 末端的 X-H 键中方便地一锅法引入不同的芳基。Pt 试剂还可用于进一步芳基化 Lys 和 Trp 中的 N-H 键，从而得到含有多个芳基的肽。
