On April 27, 2000, Almansa, Carmen; Gonzalez, Concepcion; Torres, M<
Title compounds I are disclosed [wherein one of X or Y = N; other = C; R1 = H, Me, halo, cyano, NO2, CHO, COCH3 or COOR4; R2 = (un)substituted aryl or heteroaryl; R3 = C1-8 alkyl, C1-8 haloalkyl, or NR4R6; R4 = H, C1-8 alkyl, or (un)substituted aryl(alkyl); R6 = H, C1-8 alkyl, arylalkyl, COR8, or CO2R8; R8 = C1-8 alkyl or C1-8 haloalkyl; aryl = Ph or naphthyl; heteroaryl = pyridyl, pyrazinyl, pyrimidinyl, or pyridazinyl, optionally fused to a benzene ring]. The compounds are useful as selective inhibitors of cyclooxygenase-2 (COX-2), and particularly as antiinflammatories. Claimed uses include treatment of inflammation, pain, fever, prostanoid-induced smooth muscle contraction, dysmenorrhea, premature labor, asthma, bronchitis, cancer (especially gastrointestinal or colon), cerebral infarct, epilepsy, or neurodegenerative diseases such as Alzheimer’s disease or dementia. For instance, 4-(MeSO2)C6H4NH2 was condensed with 4-FC6H4CHO under Dean-Stark conditions, and the resulting imine was cyclized with tosylmethyl isocyanide (75%), followed by imidazole ring chlorination with N-chlorosuccinimide (80%), to give the invention compound II. This compound gave 89% inhibition of COX-2 at 1 μM in vitro, but only 37.8% inhibition of COX-1 at 10 μM. The experimental process involved the reaction of Ethyl 3-fluoro-4-methylbenzoate(cas: 86239-00-1).Safety of Ethyl 3-fluoro-4-methylbenzoate
The Article related to imidazole preparation antiinflammatory cox2 inhibitor, cyclooxygenase 2 inhibitor imidazole preparation, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Safety of Ethyl 3-fluoro-4-methylbenzoate
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