作者:Rushia A. Turner、Robert J. Weber、R. Scott Lokey
DOI:10.1021/ol100471k
日期:2010.4.16
A mild and effective method was developed to convert peptides immobilized on the 2-chlorotrityl and Wang resins directly to C-terminal esters. After conventional Fmoc peptide synthesis, treatment with anhydrous HCl (0.2−3 M) in a variety of alcohols was shown to produce the corresponding peptide esters in good yield and purity. Under the mildest conditions investigated, acid-sensitive protection groups
开发了一种温和有效的方法,将固定在2-氯三苯甲基和Wang树脂上的肽直接转化为C端酯。在常规的Fmoc肽合成后,显示在各种醇中用无水HCl(0.2-3 M)处理可产生相应的肽酯,并具有良好的收率和纯度。在最温和的条件下,对酸敏感的保护基团(如N -Boc,三苯甲基,叔丁基醚,叔丁酯和Pbf)保持完整。