Assembly of Nitrated Isoxazoles via a Multicomponent Cascade Reaction Using Benzoxathiazine-2,2-dioxides as C1
Xian Liu1, Xiao Yu1, Shengkui Jin1
1Engineering Research Center of Pharmaceutical Process Chemistry, Ministry of Education, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, P. R. China.
Abstract:
A novel multicomponent cascade reaction involving benzoxathiazine-2,2-dioxides, styrenes, and sodium nitrite has been developed. This method provides a facile and practical one-pot route to nitrated isoxazoles under transition-metal-free conditions. Notably, it first utilizes benzoxathiazine-2,2-dioxides as C1 synthons and exhibits excellent regioselectivity. Moreover, the introduced phenolic hydroxyl groups in the products offer promising handles for further structural diversification, enhancing their potential for active drug development.
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