Late‐Stage Diversification of Non‐Steroidal Anti‐Inflammatory Drugs by Transition Metal‐Catalyzed C–H Alkenylations, Thiolations and Selenylations

Abstract

Abstract Ruthenium‐ and silver‐catalyzed selective C–H alkenylations, thiolations and selenylations of phenazone (antipyrine) – a non‐steroidal anti‐inflammatory drug – have been developed. This method features ample substrate scope, affording typically the mono‐ ortho alkenylated, thiolated and selenylated products in good yields with complete site selectivity control. This strategy offers an efficient protocol for the modification of antipyrine derivatives. magnified image