A kind of medicine for treating hepatitis B and its preparation method
A pharmacy and compound technology, applied in the field of medicine, can solve the problems of poor curative effect, easy recurrence of drug withdrawal, drug resistance, etc., and achieve the effects of good inhibitory effect, excellent anti-hepatitis B virus activity, and low toxicity.
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Embodiment 1
[0047] Example 1: (E)-3-((5-methylpyrimidin-4-yl)methylene)-6-(pyrrolidin-1-ylmethyl)isoindol-1-one (MIDO-1 )Synthesis
[0048]
[0049] Step 1: Mix 3.71 g of 6-(bromomethyl)isoindol-1-one, 1.42 g of tetrahydropyrrole, and 7.31 g of cesium carbonate in 50 mL of THF under a nitrogen atmosphere at -5°C. The reaction solution was warmed to room temperature and stirred overnight. The resulting solution was diluted with 200 mL water and then extracted with 3×100 mL ethyl acetate. The combined organic layer was washed once with 100 mL water and 100 mL brine each and dried over anhydrous calcium chloride. The solvent was removed by rotary evaporation, and the residue was purified by silica gel column chromatography (ethyl acetate: petroleum ether = 1:5) to obtain 3.17 g of intermediate 6-(pyrrolidin-1-ylmethyl)isoindol-1-one , The yield is 89.0%.
[0050] ESI-MS: 217.13[M+H] +
[0051] Step 2: Dissolve 1.46g of 5-methylpyrimidine-4-carbaldehyde in 150ml of absolute ethanol, then add 2....
Embodiment 2
[0055] Example 2: (E)-3-((6-hydroxypyrimidin-4-yl)methylene)-6-(piperazin-1-ylmethyl)isoindol-1-one (MIDO-2) Synthesis
[0056]
[0057] Step 1: Mix 3.71 g of 6-(bromomethyl)isoindol-1-one, 1.72 g of piperazine, and 7.31 g of cesium carbonate in 80 mL of THF at -5°C under a nitrogen atmosphere. The reaction solution was warmed to room temperature and stirred overnight. The resulting solution was diluted with 200 mL water and then extracted with 3×100 mL ethyl acetate. The combined organic layer was washed once with 100 mL water and 100 mL brine each and dried over anhydrous calcium chloride. The solvent was removed by rotary evaporation, and the residue was purified by silica gel column chromatography (ethyl acetate:n-hexane=1:3) to obtain 3.33 g of intermediate 6-(piperazin-1-ylmethyl)isoindol-1-one , The yield is 87.3%.
[0058] ESI-MS: 232.14[M+H] +
[0059] Step 2: Dissolve 1.48g of 6-hydroxypyrimidine-4-carbaldehyde in 100ml of absolute ethanol, then add 2.32g of 6-(piperaz...
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