Continuous Flow Processes as an Enabling Tool for the Synthesis of Constrained Pseudopeptidic Macrocycles
作者:Ferran Esteve、Raul Porcar、Santiago V. Luis、Belen Altava、Eduardo García-Verdugo
DOI:10.1021/acs.joc.1c03081
日期:2022.3.4
4-f]-isoindolocyclophane scaffold and involving four coupled substitution reactions in the macrocyclization process. Appropriate design of a supported base permitted the continuous production of the macrocycles even at large scales, taking advantage of the positive template effect promoted by the bromide anions. In addition, the use of flow protocols allowed a ca. 20-fold increase in productivity as well as reducing
在此,我们报告了我们为开发一种连续流动方法而做出的努力,该方法可有效制备含有六氢吡咯并-[3,4- f ]-异吲哚并环芳基骨架的伪肽大环化合物,并在大环化过程中涉及四个偶联取代反应。利用溴化物阴离子促进的正模板效应,即使在大规模情况下,适当设计的支撑碱基也可以连续生产大环化合物。此外,流协议的使用允许 ca。与相关的批量大环化工艺相比,生产率提高 20 倍,环境影响降低近 2 个数量级。