52535-35-0Relevant articles and documents
A convenient synthesis of the key intermediate of selective COX-2 inhibitor Etoricoxib
Tartaggia, Stefano,Caporale, Andrea,Fontana, Francesco,Stabile, Paolo,Castellin, Andrea,De Lucchi, Ottorino
, p. 18544 - 18549 (2013/10/21)
An original strategy for the synthesis of ketone 1, the key intermediate for preparing Etoricoxib, an important nonsteroidal anti-inflammatory drug, has been developed. Inexpensive 5-hydroxy-2-methylpyridine was converted to the corresponding acetyl derivative in four practical synthetic steps. The following palladium-catalyzed α-arylation of acetylpicoline with 4-bromo- or 4-chlorophenyl methyl sulfone was efficiently optimized in order to afford ketone 1 in remarkable yield.
