Lee Hong-Kee, Cao Hong, Rana Tariq M
Program in Chemical Biology, Department of Biochemistry and Molecular Pharmacology, University of Massachusetts Medical School, 364 Plantation Street, Worcester, Massachusetts 01605, USA.
J Comb Chem. 2005 Mar-Apr;7(2):279-84. doi: 10.1021/cc0498480.
A highly efficient microwave-assisted method was successfully developed for the synthesis of a library of carbostyril analogues. The reaction time for synthesis of carbostyril analogues was drastically reduced from a reported 18-58 h to only 80 min. Compounds obtained directly from each synthesis were more than 90% pure and did not require any further purification. On the basis of the fluorescence spectra of the compounds in the initial library, four carbostyril analogues were designed. Two of these analogues showed very favorable fluorescence profiles and have the potential to be used as small molecule organic antennas for LRET studies.
成功开发了一种高效的微波辅助方法用于合成咔唑酮类似物库。咔唑酮类似物的合成反应时间从报道的18 - 58小时大幅缩短至仅80分钟。每次合成直接得到的化合物纯度超过90%,无需进一步纯化。根据初始库中化合物的荧光光谱,设计了四种咔唑酮类似物。其中两种类似物显示出非常良好的荧光特性,有潜力用作LRET研究的小分子有机天线。