Arai Takayoshi, Mizukami Tomoe, Yanagisawa Akira
Department of Chemistry, Faculty of Science, Chiba University, Inage 263-8522, Japan.
Org Lett. 2007 Mar 15;9(6):1145-7. doi: 10.1021/ol0702122. Epub 2007 Feb 22.
Catalytic asymmetric benzoylation of 1,2-diols has been developed using a solid-phase asymmetric catalyst. The reaction conditions were optimized by the screening of different metal salts, solvents, bases, and temperatures. High-throughput screening was performed using circular dichroism detection, and the results revealed that Nb-imidazoline-copper(I) in combination with diisopropylethylamine was able to catalyze with high enantioselectivity, giving the monobenzoylated products in high yields and excellent enantiomeric excesses of up to 95% ee. [reaction: see text]
已开发出使用固相不对称催化剂对1,2 -二醇进行催化不对称苯甲酰化反应。通过筛选不同的金属盐、溶剂、碱和温度对反应条件进行了优化。使用圆二色性检测进行高通量筛选，结果表明，铌 - 咪唑啉 - 铜（I）与二异丙基乙胺组合能够以高对映选择性进行催化，以高收率得到单苯甲酰化产物，对映体过量高达95%ee。[反应：见正文]
