2-(4-carbamoyl)anilino-4-aminopyrimidine derivatives and their applications
A carbamoyl and aminopyrimidine technology, applied in the field of 2-anilino-4-aminopyrimidine derivatives and applications, can solve the problems of few reports in research, achieve good application prospects, high yield, and significant anti-tumor activity Effect
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[0032] Synthesis of 2-(4-carbamoyl)anilino-4-aminopyrimidine derivatives
[0033] (1) Synthesis of intermediate 2 (N-methyl-4-nitrobenzamide):
[0034] synthetic route:
[0035]
[0036] Synthesis process: take 250mL dry reactor, add 4-nitrobenzoic acid (1g, 6mmol), then add 30mL oxalyl chloride to dissolve, stir reaction on an oil bath at 65-70°C (anhydrous operation), and wait for the solution When it became a light yellow transparent liquid, the solution was spin-dried under reduced pressure to obtain a yellow solid; the yellow solid was dissolved in dichloromethane, and triethylamine (1.8 g, 178 mmol) was slowly added in an ice bath, and then 40% methylamine aqueous solution ( 287mg, 5.2mmol), stirred at room temperature for about 30 minutes; after the reaction was complete, the solvent was spin-dried under reduced pressure, the spin-dried mixture was dissolved with ethyl acetate and an appropriate amount of water and the solution was extracted with ethyl acetate for 5...
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