Institute for Glycomics, Gold Coast Campus, Griffith University, QLD 4222, Australia.
Org Biomol Chem. 2019 Jan 23;17(4):803-806. doi: 10.1039/c8ob02696c.
Amidine synthesis by amine addition to nitriles normally requires high temperatures or harsh catalysts. Here, we report that boronate esters can facilitate amidination of proximal amines with moderate heating. With amidines present in a number of drugs and the synthetic handle provided by the boron, this chemistry should find useful applications.
伯硼酸酯可以促进邻位胺与腈的酰胺化反应,在温和加热的条件下即可进行,而通常情况下,胺与腈的酰胺化反应需要高温或苛刻的催化剂。酰胺键存在于许多药物中,而硼原子又提供了一个合成片段,因此该反应具有很大的应用潜力。