2,4-di-substituted amido-6-substituted-[1,3,5]triazine or miazines compound, preparation method, pharmaceutical combination and use of the same
A two-substituted, compound technology, applied in the fields of medicinal chemistry and pharmacotherapy, can solve the problems of HIV virus resistance reverse transcriptase and protease inhibitors, side effects, false positives, and unclear mechanisms, and achieve inhibition of virus replication. Effect
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Embodiment 1
[0131] 4,6-dichloro-[1,3,5]triazin-2-ylaniline (II-1)
[0132]Dissolve 2.0 g of 2,4,6-trichloro-[1,3,5]triazine in 12 ml of dioxane, and slowly add aniline in acetone solution (1 g / 2 ml) with stirring in an ice bath ). After the dropwise addition was completed, 1.16 g of sodium carbonate was added at one time, and the mixture was stirred in an ice bath for 5 hours, then warmed up to room temperature and stirred for 2 hours. 150 ml of water was added dropwise to the reaction solution, stirred for 30 minutes, a large amount of solid was precipitated, filtered with suction, washed with water, and dried to obtain 2.48 g of a light yellow solid product with a yield of 95.4%. Mp 132-133°C (lit. 133-135°C). MS-EI 240 (M+, 100%).
Embodiment 2
[0134] (4-Chloro-6-morpholin-4-yl-[1,3,5]triazin-2-yl)aniline (III-1)
[0135] Dissolve 1.0 g of II-1 in 6 ml of dioxane, and slowly add a solution of morpholine in acetone (0.36 g / 1 ml) dropwise under cooling and stirring in an ice bath. After the dropwise addition, 0.438 g of sodium carbonate was added at one time, and the mixture was stirred in an ice bath for 2 hours, then warmed up to room temperature and stirred for 1 hour. 70 ml of water was added dropwise to the reaction solution, stirred for 30 minutes, a large amount of solid was precipitated, filtered with suction, washed with water, and dried to obtain 1.06 g of a light yellow solid product with a yield of 88.0%. Mp 193-195°C (lit. 198.5-199.5°C). 1H-NMR (400Hz, CDCl3) δ: 3.75 (4H, m), 3.85 (4H, m), 7.14 (1H, t), 7.18 (1H, br), 7.38 (2H, t), 7.52 (2H, t ).
Embodiment 3
[0137] (4-hydrazino-6-morpholin-4-yl-[1,3,5]triazin-2-yl)aniline (IV-1)
[0138] Put 0.5 g of III-1 into 15 ml of 85% hydrazine hydrate, reflux and stir for 2 hours, cool to room temperature, pump up, and wash with a small amount of absolute ethanol to obtain 0.4 g of off-white solid with a yield of 81.6%. Mp 170-171°C; MS-EI 287 (M+, 100%).
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