天然产物在药物化学中具有非常重要的地位,天然产物杂合物的设计合成,可以为药物筛选提供数目更多、结构更多样化的生物活性分子,是发现更多的新药先导化合物的一条非常重要的途径.以邻苯二甲醚为原料,经傅克酰基化、酮酯缩合、Knoevenagel缩合、Nazarov环化、酮酸酯的胺解、1,3-二羰基化合物的α-羟基化、酮羰基和酰胺的还原及分子内的傅克环化共9步反应,合成了氮杂brazilin(Aza-brazilin)与1,3-二芳基茚类化合物的一个杂合物.
Natural products play the most important role in the development of drugs.The design and synthesis of natural products hybrids seem to be a promising approach to increase the number and the diversity of compounds for pharmacological testing and were expected to disclose an avenue toward the development of valuable leads for medicinal applications.In this paper the synthesis of an aza-brazilin/1,3-diarylindan-based hybrid starting from 1,2-dimethoxy-benzene was reported.The synthesis finished in 9 steps including Friedel-Crafts acylation,Claisen condensation,Knoevenagel condensation,Nazarov cyclization,aminolysis of β-keto esters,α-hydroxylation of β-dicarbonyl compounds,reduction of ketone,amide and the in-tra-molecular Friedel-Crafts cyclization reaction.