一种通过一锅法炔烃-叠氮环加成反应合成三唑并苯二氮䓬衍生物的简洁路线。
A concise route to triazolobenzodiazepine derivatives via a one-pot alkyne-azide cycloaddition reaction.
作者信息
Thomas Andrew W
机构信息
F. Hoffmann-La Roche AG, Pharmaceuticals Division, Discovery Chemistry, Basel, CH 4070, Switzerland.
出版信息
Bioorg Med Chem Lett. 2002 Jul 22;12(14):1881-4. doi: 10.1016/s0960-894x(02)00262-7.
Abstract
A new and efficient one-pot synthesis of [1,2,3]triazolo[1,5-a][1,4] benzodiazepin-6(4H)-ones is described starting from readily available anthranilic acids. A small array of the title compounds were assembled via a four-step sequence involving diazotisation, azide addition followed by amide bond formation employing polymer supported carbodiimide and subsequent 1,3-dipolar cycloaddition reaction.
摘要
描述了一种从容易获得的邻氨基苯甲酸开始的新型高效一锅法合成[1,2,3]三唑并[1,5 - a][1,4]苯并二氮杂䓬 - 6(4H)-酮的方法。通过一个四步序列组装了一小批目标化合物，该序列包括重氮化、叠氮化物加成，随后使用聚合物负载的碳二亚胺形成酰胺键，以及随后的1,3 - 偶极环加成反应。
Zotero 插件