Synthesis of Novel Anticancer Agents

描述(申请人提供)：考虑到这一领域的最新发展，具有戊二酮和金丝桃素结构类型的光动力癌症治疗的潜力尤其值得注意。拟议的计划重点是通过模拟生物氧化系统来合成这种复杂的天然产物及其类似物。将利用手性氧化催化剂开发在建立轴向手性的同时通过氧化C-H键激活形成C-C键的方法。对于复杂的底物，在这些转化中选择性的可能性具有很大的合成潜力。如果实现了这些目标，就可以设想用于天然产品组装的新颖和独特的合成策略。介绍了合成对称和不对称手性联苯并二酮、并二苯二酮、双萘并吡喃、双并蒽醌、金丝桃素和双黄酮类天然产物的路线。

DESCRIPTION (provided by applicant): The potential for photodynamic cancer therapy with the perylenequinone and hypericin structural types is especially noteworthy given recent developments in this area. The proposed program focuses on synthesis of such complex natural products and their analogs by mimicking biological oxidative systems. Methods to form C-C bonds via oxidative C-H bond activation while establishing axial chirality will be developed using chiral oxidative catalysts. The possibility of selectivity in these transformations with respect to complex substrates is of significant synthetic potential. If such goals are realized, novel and unique synthetic strategies for the assembly of natural products can be envisioned. Routes to symmetric and dissymmetric chiral binaphthyl, perylenequinone, bisnaphthopyrone, bisanthraquinone, hypericin, and bisflavone natural products are presented.