通过在流动相中精确控制快速异构化反应实现α-官能化二苯乙烯的区域选择性合成。
Regioselective Synthesis of α-Functional Stilbenes via Precise Control of Rapid - Isomerization in Flow.
机构信息
Department of Chemistry, College of Science, Korea University, Seongbuk-gu, Seoul 02841, South Korea.
Department of Synthetic and Biological Chemistry, Graduate School of Engineering, Kyoto University, Nishikyo-Ku, Kyoto 615-08510, Japan.
出版信息
Org Lett. 2021 Apr 16;23(8):2904-2910. doi: 10.1021/acs.orglett.1c00538. Epub 2021 Apr 2.
The rapid - isomerization of α-anionic stilbene was regioselectively controlled by using flow microreactors, and its reaction with various electrophiles was conducted. The reaction time was precisely controlled within milliseconds to seconds at -50 °C to selectively give the - or -isomer in high yields. This synthetic method in flow was well-applied to synthesize precursors of commercial drug compound, ()- and ()-tamoxifen with high regioselectivity and productivity.
使用流微反应器，可对α-阴离子二苯乙烯的快速异构化进行区域选择性控制，并与各种亲电试剂进行反应。在-50°C 下，反应时间精确控制在毫秒至秒级，以高收率选择性地得到β-或γ-异构体。这种在流中的合成方法很好地应用于商业药物化合物（）-和（）-他莫昔芬的前体的高区域选择性和高生产率合成。
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