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Synthesis of benz[d]indeno[1,2-b]pyran-5,11-diones: versatile intermediates for the design and synthesis of topoisomerase I inhibitors.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2006 Apr 1 , DOI: 10.1016/j.bmcl.2006.01.008
Andrew Morrell , Smitha Antony , Glenda Kohlhagen , Yves Pommier , Mark Cushman

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.

中文翻译:

苯并[d]茚并[1,2-b]吡喃-5,11-二酮的合成:用于设计和合成拓扑异构酶I抑制剂的通用中间体。

已开发出一种方法,该方法依靠邻苯二甲酸酯和2-羧基苯甲醛之间的两步一锅缩合以多克形式提供苯并[d]茚并[1,2-b]吡喃-5,11-二酮。用伯胺处理这些化合物可以快速获得各种N-取代的茚并异喹啉,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。
更新日期:2017-01-31
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