important benzimidazole building block BYK308944 was elaborated using the Stobbe reaction as central element. BYK308944 constitutes an important intermediate for the preparation of 3,6,7,8-tetrahydrochromeno[7,8-d]imidazoles as potassium-competitive acid blockers. The new route relies on the hydroxymethylation of 1,2-dimethylimidazole as cheap starting material followed by oxidation of the corresponding alcohol
重要的
苯并咪唑结构单元BYK308944的全新合成工艺以Stobbe反应为中心元素。BYK308944构成了一种重要的中间体,用于制备3,6,7,8-四氢
色酚[7,8- d ]
咪唑类化合物,作为
钾竞争性酸阻滞剂。新途径依赖于
1,2-二甲基咪唑作为廉价的原料进行羟甲基化,然后氧化相应的醇,然后将所得醛与
琥珀酸二乙酯进行Stobbe缩合反应。此新方法的所有合成步骤均经过优化,目的是建立适合大规模制备的工艺。