Protein Kinase Targeted Therapeutics
a protein kinase and targeted technology, applied in the field of protein kinase targeted therapeutics, can solve the problems of previous inhibitors having problems directly or indirectly related to the molecular properties of compounds, and the target (e.g., inhibiting) intracellular protein kinases
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[0070]FIG. 1 shows different exemplary routes of synthesis for the compounds, small molecules, and analogs thereof of the present invention.
[0071] 1-Phenyl-2-(pyridin-4-yl)ethanone: (2) To a stirred solution of lithium diisopropylamide (1.5 eq) in THF at −78° C. a solution of 4-picoline (1 eq) in THF is added slowly. After 15 min, a solution of N-methoxy-N-methylbenzamide (1.2 eq) in THF is added. The reaction mixture is allowed to warm to ambient temperature. The formation of product is monitored by HPLC. The reaction mixture is poured into a saturated aqueous sodium bicarbonate solution, then extracted with ethylacetate. The organic phase is washed with brine, dried over anhydrous magnesium sulphate and evaporated under reduced pressure to give the crude product. The crude product is then purified by flash column chromatography (25-100% EtOAc-hexane) to give the product ketone 2. Purity >90%, ESI m / z 198.18 (MH+).
[0072] Ethyl 4-oxo-4-phenyl-3-(pyridin...
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