Institute of Biostructures and Bioimaging, National Research Council, 80134 Naples, Italy.
Department of Chemistry and Biochemistry, University of Colorado , Boulder, Colorado 80309, United States.
Org Lett. 2015 Nov 20;17(22):5646-9. doi: 10.1021/acs.orglett.5b02931. Epub 2015 Nov 2.
A solid-phase S-alkylation procedure to introduce chemical modification on the cysteine sulfhydryl group of a peptidyl resin is reported. The reaction is promoted by activated molecular sieves and consists of a solid-solid process, since both the catalyst and the substrate are in a solid state. The procedure was revealed to be efficient and versatile, particularly when used in combination with the solution S-alkylation approach, allowing for the introduction of different molecular diversities on the same peptide molecule.
本文报道了一种在肽树脂的半胱氨酸巯基上进行化学修饰的固相 S-烷基化方法。该反应由活性分子筛促进,是一个固-固过程,因为催化剂和底物都处于固态。该方法被证明是高效和通用的,特别是与溶液 S-烷基化方法结合使用时,可以在同一肽分子上引入不同的分子多样性。