Department of Chemistry and Biochemistry, National Chung Cheng University, Minhsiung, Chiayi, Taiwan, ROC.
Org Lett. 2011 Mar 4;13(5):920-3. doi: 10.1021/ol1029707. Epub 2011 Jan 26.
Starting with inexpensive reagents, a self-directed chemical process with the aid of a single metal triflate was readily achieved to concomitantly construct quinazoline and pyrroloquinoline cores to afford the synthesis of luotonin A and its analogues. Among all compounds prepared, 2c, 2d, and 3b exhibit more potent inhibitory activity than luotonin A against human topoisomerase I.
以廉价试剂为起始原料,在单金属三氟甲磺酸酯的辅助下,通过一个自导向的化学过程,可同时构建喹唑啉和吡咯并喹啉核心,从而实现洛洛西汀 A 及其类似物的合成。在所制备的所有化合物中,化合物 2c、2d 和 3b 对人拓扑异构酶 I 的抑制活性强于洛洛西汀 A。