Synthesis and molecular structure of 1-(pyrimidin-2-yl)-2-(4-aryl-1,3-thiazol-2-yl)hydrazines

Synthesis and Investigation of Phthalazinones as Antitubercular Agents

“…Finally, the assembly of pyrimidinyl‐phthalazinones was undertaken. First, the chloropyrimidines were synthesised via the treatment of guanidine carbonate ( 33 ) with either ethyl acetoacetate ( 34 ), ethyl benzoylacetate ( 35 ), or ethyl‐4‐fluorobenzoylacetate ( 36 ) to give hydroxypyrimidines 37 , 38 , and 39 , respectively, in good yield (Scheme A). The hydroxypyrimidines were then treated with POCl 3 under heating with reflux to yield the corresponding chloropyrimidines 40 , [40 ] 41 and 42 .…”

“…Finally,t he assemblyo fp yrimidinyl-phthalazinonesw as undertaken. First, the chloropyrimidines weres ynthesised via the treatment of guanidine carbonate (33)w ith either ethyl acetoacetate (34), [40] ethyl benzoylacetate (35), [41] or ethyl-4-fluoro-Scheme1.Retrosynthesis for the preparation of pyrimidinyl-phthalazinones (II)and phthalazinones (I).…”

“…2019, 14,1278 -1285 www.chemasianj.org benzoylacetate (36)t og ive hydroxypyrimidines 37, 38,a nd 39, respectively,i ng ood yield (Scheme 4A). The hydroxypyrimidines weret hen treated with POCl 3 under heating with reflux to yield the corresponding chloropyrimidines 40, [40] 41 [42] and 42.C ondensation of the chloropyrimidines with amino-phthalazinones 27, 30 and 32 under acidic conditions then gave pyrimidinyl-phthalazinones 43-51 in moderate to good yields (Scheme4B). Successful formation of pyrimidinyl-phthalazinones 43-51 was confirmedv ia NMR spectroscopy,w hich includeda nH MBC betweent he bridging amine NH and carbons at the 5'-, 8-and 6-positions.…”

MNPs@SiO2‐Pr‐AP: A new catalyst for the synthesis of 2‐amino‐4‐aryl thiazole derivatives

“…In recent years, the solvent‐free organic reactions have captured great interests owing to their many advantages including high efficiency and selectivity, easy separation and purification, mild reaction conditions, reduction in wastes, and benefits to the industry and environment . In recent decades, heterocyclic compounds have attracted much attention because of their abundance, and their increasing importance in the field of pharmaceuticals and chemical industries . Thiazole and its derivatives have been shown to possess a broad range of biological activities.…”

“…[1] In recent decades, heterocyclic compounds have attracted much attention because of their abundance, and their increasing importance in the field of pharmaceuticals [2] and chemical industries. [3] Thiazole and its derivatives have been shown to possess a broad range of biological activities. For example, thiamine is known as vitamin B 1 , Ritonavir is an anti-HIV agent, and Nizatidine is an anti-acid agent for the treatment of gastroesophageal reflux disease (Figure 1).…”