- Pyrimidine-containing tri-substituted imidazole compound and application thereof
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The invention relates to a pyrimidine-containing tri-substituted imidazole compound and application thereof. The compound has a structure shown as a formula (I). The compound can be used for effectively inhibiting EGFR (epidermal growth factor receptor) C797S mutation including EGFR ex19del/T790M/C797S and L858R/T790M/C797S; meanwhile, the compounds also have high inhibitory activity on single-point mutation L858R, ex19del and double-point mutation such as L858R/T790M, ex19del/T790M and the like, and moreover, the compounds have a weak inhibitory effect on wild EGFR (epidermal growth factor receptor), namely, the compounds have very good selectivity. The compound has potential to become a drug for treating malignant tumors carrying EGFR C797S mutation, especially non-small cell lung cancer(NSCLC), and has great application value.
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Paragraph 0386; 0387
(2020/07/15)
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A new method for the meta acylation of anisole and its para-methyl or fluoro derivatives, is described. Addition of two trimethysilyl groups in the 2 and 5 positions (relative to the methoxy group), followed by hydrolysis affords the corresponding 5-trimethylsilyl-3-cyclohexenones. Electrophilic substitution of the silyl group using RCOC1/2AlCl3 at low temperature provides, after final aromatisation promoted by Pd/C or CuBr2/LiBr, the expected meta acylated products. This mode of meta functionalization has been successfully applied to an original synthesis of ketoprofen starting from anisole.
- Bennetau,Rajarison,Dunogues
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p. 1179 - 1188
(2007/10/02)
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