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A Simple Protocol for the Stereoselective Construction of Enaminyl Sulfonyl Fluorides

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journal contribution
posted on 14.05.2020, 19:07 by Jing Leng, Wenjian Tang, Wan-Yin Fang, Chuang Zhao, Hua-Li Qin
A clickable connective hub 1-bromo-2-triazolethane-1-sulfonyl fluoride BTESF (1) was developed and successfully applied for the fluorosulfonylvinylation of a host of primary and secondary cyclic or acyclic amines including amino acids and pharmaceuticals. Further antimicrobial experiments revealed that vinyl sulfonyl fluoride functionalized norfloxacin (3ak), ciprofloxacin (3am), and lomefloxacin (3an) exhibited 4-fold improved antimicrobial activity against Gram-positive bacteria compared to their parent drugs.