Total synthesis of landomycins Q and R and related core structures for exploration of the cytotoxicity and antibacterial properties
作者:Yao-Hsuan Lai、Soumik Mondal、Hsin-Tzu Su、Sheng-Cih Huang、Mine-Hsine Wu、I.-Wen Huang、Tsai-Ling Yang Lauderdale、Jen-Shin Song、Kak-Shan Shia、Kwok-Kong Tony Mong
DOI:10.1039/d1ra01088c
日期:——
Herein, we report the total synthesis of landomycins Q and R as well as the aglycone core, namely anhydrolandomycinone and a related core analogue. The synthesis features an acetate-assisted arylation method for construction of the hindered B-ring in the core component and a one-pot aromatization–deiodination–denbenzylation procedure to streamline the global functional and protecting group manuipulation
在此,我们报道了兰霉素 Q 和 R 以及苷元核心(即脱水兰霉素酮和相关核心类似物)的全合成。该合成采用乙酸酯辅助芳基化方法来构建核心成分中的受阻B环,并采用一锅芳构化-脱碘-去苄基化程序来简化整体功能和保护基团的操作。随后的细胞毒性和抗菌研究表明,landomycin R 是一种针对耐甲氧西林金黄色葡萄球菌的潜在抗菌剂。