A.V. Topchiev Institute of Petrochemical Synthesis, Russian Academy of Science, 29, Leninsky Avenue, Moscow 119991, Russia.
Org Lett. 2010 Sep 3;12(17):3894-7. doi: 10.1021/ol101590w.
A novel and efficient method for the synthesis of heteroannulated [1,4]benzodiazepines via an isocyanide-based multicomponent reaction is reported. The tetrazolo[1,5-a][1,4]benzodiazepines were obtained by a facile azide Ugi five-center four-component reaction (U-5C-4CR) using ketones, sodium azide, ammonium chloride, and corresponding isocyanide. The aforementioned tetrazolodiazepines represent a notable class of compounds with proven platelet aggregation inhibitory and cholecystokinin agonist activities.
报道了一种通过异氰基多组分反应合成杂环并[1,4]苯并二氮杂卓的新颖有效的方法。通过酮、叠氮化钠、氯化铵和相应的异氰化物的简便叠氮 Ugi 五中心四组分反应（U-5C-4CR）获得了四唑并[1,5-a][1,4]苯并二氮杂卓。上述四唑并二氮杂卓是一类具有已证明的血小板聚集抑制和胆囊收缩素激动活性的显著化合物。
