Department of Chemistry, Gakushuin University, Mejiro, Toshima-ku, Tokyo, Japan.
Angew Chem Int Ed Engl. 2011 Aug 22;50(35):8180-3. doi: 10.1002/anie.201103240. Epub 2011 Jul 11.
Amines to an end: highly optically active α-CF(3)-functionalized amines can be obtained using metal-free reaction conditions. The method involves the transfer hydrogenation of CF(3)-substituted ketimines catalyzed by 1 and reductive amination of CF(3)-substituted ketones. The synthetic utility of this method was demonstrated by the synthesis of a CF(3) analogue of NPS R-568. PMP=para-methoxyphenyl.
在无金属条件下,可通过转移氢化反应,高效地获得手性α-CF(3)-官能化胺。该方法涉及在 1 的催化作用下,对 CF(3)-取代的亚胺进行转移氢化,以及对 CF(3)-取代的酮进行还原胺化。该方法的合成实用性通过 NPS R-568 的 CF(3)类似物的合成为例得到了证明。PMP=对甲氧基苯基。