作者:Sunil Sagar、Ivan Green
DOI:10.1055/s-0028-1087975
日期:——
Diospyrin and its analogues have been known for their antimycobacterial properties. Significant efforts have been made towards the synthesis of structural analogues of diospyrin with improved biological activities. We report here the synthesis of four novel analogues of diospyrin via a Suzuki cross coupling between bromonaphthoquinones and aryl- or naphthylboronic acids in the presence of tetrakis(triphenylphosphine)palladium(0) as catalyst, followed by selective demethylation of the intermediates.
已知diospyrin及其类似物具有抗分枝杆菌的特性。为合成具有增强生物活性的diospyrin结构类似物,人们投入了大量努力。本文报告通过溴萘醌与芳基或萘基硼酸在四(三苯基膦)钯(0)催化剂作用下进行Suzuki交叉耦合反应,随后对中间体进行选择性脱甲基化,合成了四种新型的diospyrin类似物。