摘要
以2-溴甲基-6,7-亚甲二氧基-3-喹啉酸乙酯(1)为原料,经三步合成了2-叔丁基-4-氟-苯并氧杂卓并[3,4-b]喹啉并[9,11]二氧戊环-14(6H)-酮(4)。其中,6-(2-氟-4-叔丁基-苯氧甲基)-[1,3]二氧戊环并[4,5-g]喹啉-7-羧酸是经一锅法合成的。它的分子内闭环反应是在Eaton’s reagent(P2O5-CH3SO3H)的作用下,在较温和的条件下进行的。所得新化合物3和4的结构经IR1、H NMR和元素分析得以证实。
Quinoline-fused ring many natural products and systems are a back-bone of oharma compounds and display a broad activity. For example, the cologically significant range of biological anticancer alkaloid camptothecin （Figure 1 ） is used as medicine against gastric cancer,tumors of the neck and carcinoma of the urinary bladder. Quinoline derivatives represent the major class of heterocycles, and a number of preparations have been known since the late 1980s. The quinoline skeleton is often used for the design of many synthetic compounds with diverse pharmacological properties .
出处
《化学研究与应用》
CAS
CSCD
北大核心
2008年第11期1491-1494,共4页
Chemical Research and Application
基金
辽宁省教育厅资助项目(202142037)
关键词
一锅法
喹啉
闭环
合成
伊藤试剂
one-pot reaction
quinoline
cyclization
synthesis
Eaton ＇ s reagent
