作者:Takuto Morisawa、Masaya Sawamura、Yohei Shimizu
DOI:10.1021/acs.orglett.9b02769
日期:2019.9.20
simple carboxylic acids was developed. Catalytically generated boron enolates of carboxylic acids reacted with an electrophilic aminating reagent, diisopropylazodicarboxylate, to provide amino acid derivatives. The catalysis afforded not only α-monosubstituted glycine derivatives but also α,α-disubstituted derivatives. The resulting α-aminocarboxylic acid was easily converted to carboxylic acid derivatives
开发了
硼催化的简单
羧酸的α-胺化反应。催化生成的
羧酸硼烯酸酯与亲电子胺化试剂
二异丙基偶氮二
羧酸酯反应,提供
氨基酸衍
生物。该催化不仅提供α-单取代的甘
氨酸衍
生物,而且提供α,α-二取代的衍
生物。所得的α-
氨基
羧酸易于转化为
羧酸衍
生物。通过在
硼催化剂上引入手性
配体,可以扩展至催化不对称变体。