Song Aimin, Zhang Jinhua, Lam Kit S
Division of Hematology and Oncology, Department of Internal Medicine, University of California Davis Cancer Center, 4501 X Street, Sacramento, California 95817, USA.
J Comb Chem. 2004 Jan-Feb;6(1):112-20. doi: 10.1021/cc0340022.
7-Fluoro-4-methyl-6-nitro-2-oxo-2H-1-benzopyran-3-carboxylic acid has been prepared as a novel scaffold for combinatorial synthesis of coumarins. The scaffold has three points of diversity. The optimal conditions for its reactions with different nucleophiles in solid phase were obtained. Sixteen coumarin derivatives with different structures were designed and synthesized in solid phase to demonstrate its application as a scaffold for combinatorial synthesis of coumarins. Thirteen of these derivatives were obtained in high yields. Many of these model compounds fluoresce. Combinatorial libraries constructed with this novel scaffold may have interesting biological or physical properties.
7-氟-4-甲基-6-硝基-2-氧代-2H-1-苯并吡喃-3-羧酸已被制备为用于香豆素组合合成的新型支架。该支架具有三个多样性位点。获得了其在固相中与不同亲核试剂反应的最佳条件。设计并在固相中合成了十六种不同结构的香豆素衍生物，以证明其作为香豆素组合合成支架的应用。其中十三种衍生物以高产率获得。这些模型化合物中的许多都能发出荧光。用这种新型支架构建的组合文库可能具有有趣的生物学或物理性质。
