Graduate School of Engineering, Nagoya University, Nagoya 464-8603, Japan.
Org Lett. 2013 Jul 19;15(14):3654-7. doi: 10.1021/ol401537f. Epub 2013 Jun 26.
Primary alkylboronic acids such as methylboronic acid and butylboronic acid are highly active catalysts for the dehydrative amide condensation of α-hydroxycarboxylic acids. The catalytic activities of these primary alkylboronic acids are much higher than those of the previously reported arylboronic acids. The present method was easily applied to a large-scale synthesis, and 14 g of an amide was obtained in a single reaction.
一级烷基硼酸，如甲基硼酸和丁基硼酸，是α-羟基羧酸脱水酰胺缩合反应的高效催化剂。这些一级烷基硼酸的催化活性远高于以前报道的芳基硼酸。本方法易于应用于大规模合成，在单次反应中可获得 14 克酰胺。
