Rosuvastatin calcium tablet and preparation process thereof

A technology of rosuvastatin calcium and its preparation process, which is applied in the field of rosuvastatin calcium tablets and its preparation process, can solve the problems of difficult control of product impurities, impact on product quality, high production cost, etc., so as to facilitate popularization and reduce production cost , The effect of improving productivity

Pending Publication Date: 2020-08-18
ABA CHEM CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the deficiencies of the prior art, the present invention provides a rosuvastatin calcium tablet and its preparation process, which has the advantages of simple and efficient

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment one: a kind of rosuvastatin calcium tablet, comprise following raw material: [4-[4-fluorophenyl-6-(1-methylethyl)-2-[N-methyl-(N-methyl Sulfonyl)amino]]-5-pyrimidinyl]methyltriphenylphosphine bromide, (4R-cis)-6-formyl-2,2-dimethyl-1,3-dioxane-4 - cyclopentyl acetate, potassium carbonate, dimethyl sulfoxide, toluene, acetonitrile, ethyl acetate, methanol, isopropanol, sodium hydroxide, sodium chloride and calcium chloride.

[0018] Another technical problem to be solved by the present invention is to provide a preparation process of rosuvastatin calcium tablets, comprising the following steps:

[0019] 1) Add 67.8g (0.1mol) [4-[4-fluorophenyl-6-(1-methylethyl)-2-[N-methyl-(N-methylsulfonyl) to the first reaction flask )amino]]-5-pyrimidinyl]methyltriphenylphosphine bromide, 27.0g (0.1mol)(4R-cis)-6-formyl-2,2-dimethyl-1,3-diox Hexyl-4-cyclopentyl acetate, 300mL dimethyl sulfoxide, stirred and dissolved at room temperature; and heated to 25-45 degrees Celsius;

Embodiment 2

[0023] Embodiment two: a kind of rosuvastatin calcium tablet, comprise following raw material: [4-[4-fluorophenyl-6-(1-methylethyl)-2-[N-methyl-(N-methyl Sulfonyl)amino]]-5-pyrimidinyl]methyltriphenylphosphine bromide, (4R-cis)-6-formyl-2,2-dimethyl-1,3-dioxane-4 - cyclopentyl acetate, potassium carbonate, dimethyl sulfoxide, toluene, acetonitrile, ethyl acetate, methanol, isopropanol, sodium hydroxide, sodium chloride and calcium chloride.

[0024] Another technical problem to be solved by the present invention is to provide a preparation process of rosuvastatin calcium tablets, comprising the following steps:

[0025]1) Add 67.8g (0.1mol) [4-[4-fluorophenyl-6-(1-methylethyl)-2-[N-methyl-(N-methylsulfonyl) to the first reaction flask )amino]]-5-pyrimidinyl]methyltriphenylphosphine bromide, 27.0g (0.1mol)(4R-cis)-6-formyl-2,2-dimethyl-1,3-diox Hexyl-4-cyclopentyl acetate, 300mL dimethyl sulfoxide, stirred and dissolved at room temperature; and heated to 45-75 degrees Celsius; t

Embodiment 3

[0029] Embodiment three: a kind of rosuvastatin calcium tablet, comprise following raw material: [4-[4-fluorophenyl-6-(1-methylethyl)-2-[N-methyl-(N-methyl Sulfonyl)amino]]-5-pyrimidinyl]methyltriphenylphosphine bromide, (4R-cis)-6-formyl-2,2-dimethyl-1,3-dioxane-4 - cyclopentyl acetate, potassium carbonate, dimethyl sulfoxide, toluene, acetonitrile, ethyl acetate, methanol, isopropanol, sodium hydroxide, sodium chloride and calcium chloride.

[0030] Another technical problem to be solved by the present invention is to provide a preparation process of rosuvastatin calcium tablets, comprising the following steps:

[0031] 1) Add 67.8g (0.1mol) [4-[4-fluorophenyl-6-(1-methylethyl)-2-[N-methyl-(N-methylsulfonyl) to the first reaction flask )amino]]-5-pyrimidinyl]methyltriphenylphosphine bromide, 27.0g (0.1mol)(4R-cis)-6-formyl-2,2-dimethyl-1,3-diox Hexyl-4-cyclopentyl acetate, 300mL dimethyl sulfoxide, stirred and dissolved at room temperature; and heated to 75-120 degrees Celsiu

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Abstract

The invention relates to the technical field of pharmaceutical preparations and discloses a rosuvastatin calcium tablet. [4-[4-fluorophenyl-6-(1-methylethyl)-2-[N_ methyl-(N-methylsulfonyl) amino]-5-pyrimidyl] methyltriphenylphosphonium bromide, (4R-cis)-6-formyl-2, 2-dimethyl-1, 3-dioxane-4-cyclopentyl acetate, potassium carbonate, dimethyl sulfoxide, methylbenzene, acetonitrile, ethyl acetate, methanol, isopropanol, sodium hydroxide, sodium chloride and calcium chloride. According to the rosuvastatin calcium tablet and the preparation process thereof, a plurality of experiments prove that: when reaction temperature is about 75 DEG C in intermediate synthesis, alkali is the optimal experimental condition of the potassium carbonate, and reaction raw materials can react completely, the generation of multiple impurities is prevented, productivity can be improved, and production cost is reduced; a hydrochloric acid solution is added in a rosuvastatin cyclopentyl ester synthesis process toneutralize redundant acid and alkali, so that the generation of the impurities is further reduced; and therefore, high-purity production is achieved.

Description

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Claims

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Application Information

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Owner ABA CHEM CORP
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