Department of Drug Design, University of Groningen , A. Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Org Lett. 2017 Jun 16;19(12):3195-3198. doi: 10.1021/acs.orglett.7b01324. Epub 2017 Jun 5.
A general strategy is introduced for the efficient synthetic access of disulfide linked artificial macrocycles via a Ugi four-component reaction (U4CR) followed by oxidative cyclization. The double-mercapto input is proposed for use in the Ugi reaction, thereby yielding all six topologically possible combinations. The protocol is convergent and short and enables the production of novel disulfide peptidomimetics in a highly general fashion.
本文提出了一种通用策略，通过 Ugi 四组分反应 (U4CR) 后氧化环化，高效合成二硫键连接的人工大环。双巯基输入物被提议用于 Ugi 反应，从而产生所有六种拓扑上可能的组合。该方案具有汇聚性和简短性，能够以高度通用的方式生产新型二硫键肽模拟物。
