Sanford Amberly B, Tollefson Emily J, Jarvo Elizabeth R
Department of Chemistry, University of California, Irvine, Natural Sciences II, Irvine, CA, 92697.
Isr J Chem. 2020 Mar;60:402-405. doi: 10.1002/ijch.201900071. Epub 2019 Sep 6.
A focused small library of carbamates and alcohols was prepared employing stereospecific Kumada-ring opening reactions of tetrahydropyrans. The core framework of the library members is acyclic and incorporates 1,3-substituents, to provide a conformational bias in avoiding syn-pentane interactions. A new compound with micromolar activity against MOLT-4, CCRF-CEM, and HL-60(TB) leukemia cell lines was identified from this series.
利用四氢吡喃的立体定向 Kumada 开环反应制备了一个聚焦的氨基甲酸酯和醇类小型文库。文库成员的核心骨架是无环的，并含有 1,3 - 取代基，以在避免顺式戊烷相互作用方面提供构象偏向。从该系列中鉴定出一种对 MOLT - 4、CCRF - CEM 和 HL - 60(TB)白血病细胞系具有微摩尔活性的新化合物。
