Abstract

We report an efficient method for the synthesis of 2-aryl(alkyl)-6-hydroxymethyl-4-selenoxo-4H-pyrano[2,3-e][1,3]oxazin-8-ones from the condensation of potassium selenocyanate and acyl chlorides with kojic acid in the presence of catalytic amounts of N-methylimidazole under solvent-free conditions. This new protocol offers advantages such as mild reaction conditions, short reaction time, easy work-up, and high yields of biologically active products and does not involve any hazardous solvent. This prompted us to establish a novel oxazine ring formation method to find promising bioactive oxazine compounds. They are found to have exhibit diverse pharmacological properties.

抽象的

我们报告了一种有效的方法，从硒氰酸钾的缩合反应中合成2-芳基（烷基）-6-羟甲基-4-硒代氧4-H-吡喃并[2,3- e ] [1,3]恶嗪-8-酮。在无溶剂条件下，在催化量的N-甲基咪唑存在下，用曲酸制得酰氯。该新方案具有以下优点：反应条件温和，反应时间短，易于后处理且生物活性产物的收率高，并且不涉及任何有害溶剂。这促使我们建立一种新颖的恶嗪环形成方法，以寻找有前途的生物活性恶嗪化合物。发现它们具有多种药理特性。