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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 a very important role in medicinal chemistry. The design and synthesis of natural product hybrids can provide more and more diverse bioactive molecules for drug screening, and it is one of more new drug discovery lead compounds A very important route to phthalyl ether as raw material, through the Friedel-Crafts acylation, ketoester condensation, Knoevenagel condensation, Nazarov cyclization, keto ester amine solution, 1,3-dicarbonyl compounds α-hydroxylation , The reduction of keto carbonyl and amide and the intramolecular Frieff cyclization in a total of 9 steps. A heteroconjugate of aza-brazilin and 1,3-diaryl indenes was synthesized.