用于在查尔酮衍生物中合成苯磺酰氟的氨基硫代甲酸酯介导的Selectfluor™氧化反应
Carbamothioate-mediated Selectfluor™ oxidation for the synthesis of benzenesulfonyl fluorides in chalcone derivatives.
作者信息
Jiang Boye, Zhang Juan, Wang Boning, Zhou Airui, Zou Yan, Meng Qingguo, Zhao Qingjie, Chai Xiaoyun, Gai Conghao
机构信息
School of Pharmacy, Yantai University Yantai P. R. China 264000.
Organic Chemistry Group, School of Pharmacy, Naval Medical University No. 325 Guo-he Road Shanghai 200433 P. R. China
出版信息
RSC Adv. 2025 Jun 27;15(27):22018-22022. doi: 10.1039/d5ra03427b. eCollection 2025 Jun 23.
A carbamothioate-mediated method for synthesizing benzenesulfonyl fluorides Selectfluor™ oxidation is reported, enabling compatibility with α,β-unsaturated chalcone derivatives without Michael addition side reactions. This approach offers moderate yields, broad functional group tolerance, and applications in covalent drug discovery, facilitating the incorporation of sulfonyl fluoride warheads into complex electrophilic scaffolds.
报道了一种用于合成苯磺酰氟的氨基硫代甲酸酯介导的方法，即Selectfluor™氧化法，该方法能够与α,β-不饱和查尔酮衍生物兼容，且无迈克尔加成副反应。这种方法产率适中，官能团耐受性广，可应用于共价药物发现，有助于将磺酰氟弹头引入复杂的亲电支架中。
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