N-heteroarylmethylpyrimidinamine compound, preparation method and applications thereof
A technology of heteroarylmethylpyrimidine amines and compounds, applied in the directions of botanical equipment and methods, applications, organic chemistry, etc.
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Embodiment 1
[0086] Embodiment 1 This embodiment illustrates the preparation method of compound 21 in Table 1
[0087]
[0088] 4-Chloromethyl-2-(4-methylphenyl)thiazole 1.3 dichloroacetone (170mmol), 4-methylthiobenzamide (150mmol), ethanol (150mL) and THF (75mL) at reflux and After reacting for 5-8 hours under stirring conditions. Most of the solvent was removed, cooled, the reaction solution was poured into ice water, extracted with ethyl acetate, the organic phase was washed with water, dried over anhydrous sodium sulfate, and the solvent was removed under reduced pressure to obtain 28 g of the yellow liquid title product.
[0089] 4-aminomethyl-2-(4-methylphenyl)thiazole 4-chloromethyl-2-(4-methylphenyl)thiazole (45mmol), potassium phthalimide (50mmol) React with N,N-dimethylformamide (DMF, 100mL) at 60-80°C with stirring for 2-5 hours, then cool to room temperature, pour the reaction solution into ice water, and precipitate a solid. Filter the precipitated solid, react with hydr...
Embodiment 2
[0094] Embodiment 2 This embodiment illustrates the preparation method of compound 37 in Table 1
[0095] With reference to the method of Example 1, replace 4-methylthiobenzamide in Example 1 with 2-methylthiobenzamide, and compound 5-chloro-6-ethyl-2- Methyl-N-((2-(2-methylphenyl)thiazol-4-yl)methyl)pyrimidin-4-amine (37).
Embodiment 3
[0096] Example 3 This example illustrates the preparation of compound 273 in Table 1
[0097]
[0098] 4-Chloromethyl-2-(2-methylphenyl)oxazole 1.3 dichloroacetone (150mmol) and 2-methylbenzamide (120mmol), react 3-8 at 60-120°C with stirring After 1 hour to complete, 24.9 g of the title product was obtained as a viscous solid, which was directly used in the next step.
[0099] 4-aminomethyl-2-(2-methylphenyl) oxazole 4-chloromethyl-2-(2-methylphenyl) oxazole (120mmol), potassium phthalimide ( 150mmol) and N,N-dimethylformamide (DMF, 200mL) were reacted at 60-80°C with stirring for 6-10 hours, then cooled to room temperature, and the reaction solution was poured into ice water to precipitate a solid. Filter the precipitated solid and react with hydrazine hydrate (250mmol) and ethanol (200mL) under reflux and stirring conditions for 3-5 hours, then cool and filter. After most of the ethanol was removed from the filtrate, it was extracted with ethyl acetate, the organic pha...
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