A comprehensive screening of known methods for the synthesis of coumarins was performed in order to obtain a new type of pyrrolobenzodiazepine–coumarin hybrids. A Pechmann condensation turned out to be the method of choice for successful synthesis of the desired hybrid starting from the corresponding phenol derivative and malic acid. Overall, the desired pyrrolobenzodiazepine–coumarin hybrid was obtained in a 3 step sequence starting from readily available starting materials – L-proline methyl ester and 4-methoxyanthranilic acid.

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新型吡咯并苯二氮杂-香豆素杂种的合成研究

为了获得新型的吡咯并苯并二氮杂卓-香豆素杂种，对已知香豆素合成方法进行了全面筛选。事实证明，从相应的苯酚衍生物和苹果酸开始成功合成所需杂化物的方法是Pechmann缩合反应。总的来说，所需的吡咯并苯并二氮杂卓-香豆素杂物是从容易获得的起始原料-L-脯氨酸甲酯和4-甲氧基邻氨基苯甲酸开始的，分为3个步骤。