Fraunhofer IME, Projektgruppe Bioressourcen, Gießen, Germany.
Helmholtz Zentrum München, Institut für Medizinalchemie, Hannover, Germany.
Angew Chem Int Ed Engl. 2018 Sep 10;57(37):12157-12161. doi: 10.1002/anie.201805901. Epub 2018 Aug 13.
The total synthesis of the naturally occurring antibiotic GE81112A, a densely functionalized tetrapeptide, is reported. Comparison of spectral data with those of the natural product and the lack of biological activity of the synthesized compound led us to revise the published configuration of the 3-hydroxypipecolic acid moiety. This hypothesis was fully validated by the synthesis of the corresponding epimer.
本文报道了天然抗生素 GE81112A 的全合成，这是一种具有高度官能团化的四肽。光谱数据与天然产物的比较以及合成化合物缺乏生物活性，促使我们修正了已发表的 3-羟基哌啶酸部分的构型。这一假设通过相应的差向异构体的合成得到了充分验证。
