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化学学报  2012 

8-epi-Liphagal的合成研究

DOI: 10.6023/A12090626, PP. 2232-2235

Keywords: 8-epi-Liphagal,天然产物,合成,Friedel-Crafts反应,高级中间体

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Abstract:

四环杂萜类天然产物Liphagal含有新奇的[6-7-5-6]四环骨架,是磷酸肌醇3-激酶(PI3K)的有效抑制剂之一,可以选择性抑制细胞增殖和促进细胞死亡,在治疗炎症、免疫紊乱、癌症以及心血管疾病中有潜在的医用价值.从廉价的2,4,5-三甲氧基苯甲醛出发,通过Wittig反应、Cu催化的环化反应、选择性氢化、分子内Friedel-Crafts反应,以直线步骤最长7步,8.72%的总收率实现了8-epi-Liphagal高级中间体10的合成.

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