苯并[d]茚并[1,2-b]吡喃-5,11-二酮的合成：用于拓扑异构酶I抑制剂设计与合成的通用中间体
Synthesis of benz[d]indeno[1,2-b]pyran-5,11-diones: versatile intermediates for the design and synthesis of topoisomerase I inhibitors.
作者信息
Morrell Andrew, Antony Smitha, Kohlhagen Glenda, Pommier Yves, Cushman Mark
机构信息
Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, IN 47907, USA.
出版信息
Bioorg Med Chem Lett. 2006 Apr 1;16(7):1846-9. doi: 10.1016/j.bmcl.2006.01.008. Epub 2006 Jan 25.
A method has been developed that relies on a two-step, one-pot condensation between phthalide and 2-carboxybenzaldehydes to provide benz[d]indeno[1,2-b]pyran-5,11-diones in a multi-gram fashion. Treatment of these compounds with a primary amine allows rapid access to various N-substituted indenoisoquinolines, whose in vitro anticancer activity and topoisomerase I inhibition have been evaluated.
已开发出一种方法，该方法依赖于苯酞与2-羧基苯甲醛之间的两步一锅法缩合反应，以多克规模制备苯并[d]茚并[1,2-b]吡喃-5,11-二酮。用伯胺处理这些化合物可快速获得各种N-取代的茚并异喹啉，并已对其体外抗癌活性和拓扑异构酶I抑制作用进行了评估。
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