通过钯催化、邻硝基苯甲酰胺导向的 C-H 烯丙基化反应实现β-烷基苯乙胺衍生物的动力学拆分。

School of Pharmacy, Shanghai jiaotong University, Shanghai 200240, China.

School of Pharmacy, Second Military Medical University, Shanghai 200433, China.

Molecules. 2023 Feb 15;28(4):1852. doi: 10.3390/molecules28041852.

Palladium-catalyzed C-H activation reactions have attracted the attention of organic researchers due to their unique high selectivity, broad functional group tolerance, and high efficiency, and they are widely used in natural products and asymmetric synthesis. Here, we report an example of enantioselective C-H alkenylation between -alkyl phenylethylamine compounds and styrenes with Boc-L-lle-OH as the ligand and nosylamide as the directing group. This reaction is applicable to styrene containing various electron-deficient and electron-donating substitutions and may be utilized for the synthesis of benzoazepine compounds.

钯催化的 C-H 活化反应由于其独特的高选择性、广泛的官能团容忍度和高效率而引起了有机研究人员的关注，并且它们被广泛应用于天然产物和不对称合成中。在这里，我们报告了一个使用 Boc-L-亮氨酸作为配体和邻甲苯磺酰亚胺作为导向基团的β-烷基苯乙胺化合物和苯乙烯之间的对映选择性 C-H 烯丙基化的例子。该反应适用于含有各种缺电子和供电子取代基的苯乙烯，并且可能用于苯并氮杂卓化合物的合成。