Ethyl azol-2-ylglyoxylates react smoothly with acetone in the presence of catalytic amounts of proline and trifluoroacetic acid to give the corresponding azolyl aldols in 93-98% yield. The products are easily transformed into azolyl pyridazinones in 85-98% yield by cyclization with hydrazine hydrate.
Easy Synthesis of Novel 4-Azolylpyridazin-3-ones. -A convenient two-step practical synthesis of the potential pharmacophores starts from easily accessible azolylpyruvates and acetone. -(GERASCHENKO*, O. V.; KHODAKOVSKIY, P. V.; SHIVANYUK, O. N.; SHISHKIN, O. V.; MYKHAILIUK, P. K.; TOLMACHEV, A. A.; Synthesis 2012, 8, 1263-1267, http://dx.doi.org/10.1055/s-0031-1290808 ; Enamine Ltd., Kiev 01103, Ukraine; Eng.) -Mais 32-167
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