通过取代的丁烯酮酸与醛的插烯羟醛缩合反应集体合成阿斯普维酮及其类似物。
Collective synthesis of aspulvinone and its analogues by vinylogous aldol condensation of substituted tetronic acids with aldehydes.
作者信息
Yu Xiaotan, Gu Xiaoxia, Zhao Yunpeng, Wang Fengqing, Sun Weiguang, Qi Changxing, Gu Lianghu, Zhang Yonghui
机构信息
Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology Wuhan 430030 People's Republic of China
出版信息
RSC Adv. 2023 Feb 7;13(7):4859-4864. doi: 10.1039/d2ra08133d. eCollection 2023 Jan 31.
A mild, modular and efficient synthetic method with broad substrate scope was developed for aspulvinones. Nine natural aspulvinones were synthesized, six of which were for the first time. The aldol condensation delivered -configuration products predominantly in MeCN. Meanwhile, alkoxy exchange occurred in MeOH and EtOH. Aspulvinone O and E, and substrate 49, 50, and 51 exhibited modest anti-SARS-CoV-2 activity in a high-throughput screening and enzyme kinetics assay.
我们开发了一种温和、模块化且高效的合成方法，该方法具有广泛的底物范围，用于合成曲霉醌。合成了九种天然曲霉醌，其中六种是首次合成。在乙腈中进行醛醇缩合主要生成 - 构型产物。同时，在甲醇和乙醇中发生了烷氧基交换。在高通量筛选和酶动力学测定中，曲霉醌O和E以及底物49、50和51表现出适度的抗SARS-CoV-2活性。
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