Center for Heterocyclic Compounds, Department of Chemistry, University of Florida , Gainesville, Florida 32611-7200, United States.
J Org Chem. 2014 Mar 21;79(6):2688-93. doi: 10.1021/jo500181g. Epub 2014 Mar 11.
Taurine-containing water-soluble peptidomimetics were designed and synthesized. N-terminal taurine acylations allowed synthesis of a number of taurine-containing peptides. N-protection of taurine with Cbz and SO2-activation with benzotriazole followed by coupling with various amino esters, dipeptides and nucleophiles provided taurine N- and O-conjugates and sulfonopeptides.
设计并合成了含牛磺酸的水溶性肽模拟物。通过在 N 端进行牛磺酸酰化,可以合成多种含牛磺酸的肽。用 Cbz 对牛磺酸进行 N 保护,并通过苯并三唑进行 SO2 活化,然后与各种氨基酸酯、二肽和亲核试剂偶联,得到了牛磺酸的 N-和 O-缀合物以及磺酰胺肽。