School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551.
Org Lett. 2011 Oct 7;13(19):5176-9. doi: 10.1021/ol202047q. Epub 2011 Sep 8.
An efficient "thiol switch" approach for the synthesis of peptide thioesters via an acid-catalyzed N-S acyl shift and a thioester exchange reaction in tandem with concurrent removal of protecting groups is described. This method employs novel 2-(thiomethyl)thiazolidine (TMT)-anchored resins and is fully compatible with Fmoc chemistry.
描述了一种通过酸催化的 N-S 酰基转移和硫酯交换反应串联进行，并同时去除保护基团的高效“巯基开关”方法，用于合成肽硫酯。该方法采用新型 2-（巯甲基）噻唑烷（TMT）锚固树脂，完全兼容 Fmoc 化学。
