Metal-Free Annulation of 2-Nitrobenzyl Alcohols and Tetrahydroisoquinolines toward the Divergent Synthesis of Quinazolinones and Quinazolinethiones
作者:Duc Ly、Thao T. Nguyen、Cam T. H. Tran、Vy P. T. Nguyen、Khang X. Nguyen、Phuc H. Pham、Nhan T. H. Le、Tung T. Nguyen、Nam T. S. Phan
DOI:10.1021/acs.joc.1c02017
日期:2022.1.7
synthesis of quinazolinones from commercially available 2-nitrobenzyl alcohols and tetrahydroisoquinolines is developed. The reaction conditions were tolerant of an array of functionalities such as halogen, tertiary amine, protected alcohol, and ester groups. Under nearly identical conditions, quinazolinethiones were obtained in the presence of elemental sulfur and suitable mediators.
开发了一种由市售 2-硝基苯甲醇和四氢异喹啉合成喹唑啉酮的简单无金属方法。反应条件可耐受一系列官能团,例如卤素、叔胺、受保护的醇和酯基团。在几乎相同的条件下,在元素硫和合适的介质存在下获得喹唑啉硫酮。