Cu-Catalyzed Conjugate Addition of Grignard Reagents to Thiochromones: An Enantioselective Pathway for Accessing 2-Alkylthiochromanones
作者:Qingxiong Yang、Jun Wang、Shihui Luo、Ling Meng
DOI:10.1055/s-0037-1610225
日期:2018.9
The enantioselective incorporation of alkyl groups in thiochromones was realized for the first time by a Cu/(R,S)-PPF-P t Bu2-catalyzed conjugate addition of Grignard reagents to thiochromones. With this method, a series of 2-methylthiochromanones were obtained in good yields (up to 96% yield) with moderate-to-good ee values (up to 87% ee). The established method expedites the synthesis of a large
通过Cu/(R,S)-PPF-P t Bu2 催化的格氏试剂与硫色酮的共轭加成,首次实现了烷基在硫色酮中的对映选择性掺入。使用这种方法,以良好的收率(最高 96% 的收率)获得了一系列 2-甲基硫代色满酮,其 ee 值中等至良好(最高 87% ee)。已建立的方法加速了大型手性硫代色满酮库的合成,以用于进一步的合成应用和生物学研究。