Liu Yunqi, Zhou Xiyan, Li Ruining, Sun Zhankui
Shanghai Frontiers Science Center for Drug Target Identification and Drug Delivery, School of Pharmaceutical Sciences, Shanghai Jiao Tong University, Shanghai 200240, China.
Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, Pharm-X Center, School of Pharmacy, Shanghai Jiao Tong University, No. 800 Dongchuan Rd., Shanghai 200240, China.
Org Lett. 2024 Aug 2;26(30):6424-6427. doi: 10.1021/acs.orglett.4c02232. Epub 2024 Jul 23.
The -difluoroalkene moiety is frequently found in medicinal chemistry. From α-keton sulfides and thioic acids, we were able to develop a universal approach for the synthesis of γ,γ-difluoroallylic ketones and δ,δ-difluoroallylic ketones via a desulfurative/defluorinative alkylation process. We expect that this mild and efficient method will be complementary to other known strategies.
二氟烯烃部分在药物化学中经常出现。从α-酮硫化物和硫代酸出发,我们能够通过脱硫/脱氟烷基化过程开发出一种通用的方法来合成γ,γ-二氟烯丙基酮和δ,δ-二氟烯丙基酮。我们预计这种温和且高效的方法将补充其他已知策略。