高等学校化学学报2024，Vol.45Issue(12)：57-68,12.DOI:10.7503/cjcu20240363
α-葡萄糖苷酶和人癌细胞的双效抑制剂
Optimized Synthesis of Natural Product Penasulfate A,a Dual Inhibitor Against α-Glucosidase and Human Cancer Cells
摘要
Abstract
α-Glucosidase inhibitors possess broad applications in terms of antidiabetes,anticancer,antivirus,therapy of obesity and so on.In this work,a new convergent synthetic route of Penasulfate A which is a dual inhibitor against α-glucosidase and human cancer cell lines was presented.Olefin cross-metathesis(CM),TEMPO-catalyzed oxidation,Mitsunobu reaction,copper(I)-salt catalyzed coupling reaction and Julia olefination reaction were leveraged as the key steps.The total synthesis of Penasulfate A has been completed over 10 longest linear steps with an overall yield of 13.2%,better than the previous route in which the title compound was synthesized in 14 linear steps with an 8.6%overall yield.This provides the candidate protocol for the syntheses of Penasulfate A and its analogues,along with the possibilities for the deeply investigation on their biological activities.关键词
α-葡萄糖苷酶/抑制剂/偶联反应/烯烃复分解反应Key words
α-Glucosidase/Inhibitor/Coupling reaction/Olefin cross-metathesis reaction分类
化学化工引用本文复制引用
张楠,邓昌选,林汉琳,高阳光..α-葡萄糖苷酶和人癌细胞的双效抑制剂[J].高等学校化学学报,2024,45(12):57-68,12.基金项目
国家自然科学基金(批准号:21602082)、江汉大学科技专项项目(批准号:2023KJZX06)和江汉大学双一流培育项目(批准号:2023XKZ039)资助.Supported by the National Natural Sciences Foundation of China(No.21602082),the Jianghan University Foundation,China(No.2023KJZX06)and the Excellent Discipline Cultivation Project by Jianghan University,China(No.2023XKZ039). （批准号:21602082）
