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Preparation method of sodium salt of pravastatin

A technology of naveladine sodium and naveladine, which is applied to the preparation of organic compounds, carboxylic acid ester preparation, chemical instruments and methods, etc., and can solve the problems of unhealthy operators, extremely high equipment production environment requirements, and increased investment and energy consumption issues

Active Publication Date: 2009-11-18
SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] No matter which method in the prior art, there are great disadvantages, such as the use of organic solvents is very large, which is not conducive to safety, large loss of resources and great impact on the environment
On the other hand, it is necessary to heat up the solvent to facilitate the dissolving of Naveledadine Sodium, and then cool down to crystallize Naveledadine Sodium, wherein the heating up will cause a large amount of volatilization of the organic solvent, which is very prone to serious consequences such as explosion. The requirements for equipment and production environment are extremely high, and it is not good for the health of operators; and naveladine sodium is unstable at high temperature, and high temperature will promote the degradation of naveladine sodium into other structural analogues
Cooling will inevitably increase additional cooling equipment, increasing input and operating energy consumption

Method used

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  • Preparation method of sodium salt of pravastatin
  • Preparation method of sodium salt of pravastatin
  • Preparation method of sodium salt of pravastatin

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preparation example Construction

[0043] In another preference of the present invention, the preparation method of described naveladine sodium comprises the following steps:

[0044](a) Naveladidine salt is transferred to the first solvent by extraction to form an organic solution containing naveladine; the first solvent is selected from one or more of the following groups: methyl formate, formic acid n-propyl, isopropyl formate, n-butyl formate, methyl acetate, ethyl acetate, n-propyl acetate, isopropyl acetate, n-butyl acetate, sec-butyl acetate, isobutyl acetate, tert-butyl acetate ester;

[0045] (b) adding an inorganic or organic base whose cation is a sodium ion to the organic solution obtained in step (a), to obtain a precipitate;

[0046] (c) Repeat the steps from (a) to (b) for the precipitate obtained in step (b) for 1-5 times to obtain naveladine sodium; preferably repeat 1-3 times.

[0047] In the present invention, the organic solution containing naveladidine can be obtained using methods famili...

Embodiment 1

[0071] 35 grams of naveladidine (purchased from Shanghai Tianwei Biopharmaceutical Co., Ltd.) was completely dissolved in 750 mL of ethyl acetate at 20 ° C, and then a methanol solution containing 1M NaOH was added thereto until the pH was above 7. 80 mL of methanol solution of 1M NaOH was collected by filtration and dried in vacuo to obtain 31 grams of white crystalline powder of naveladidine sodium.

[0072] The specific rotation of naveledadine sodium is +157°, the purity is 99.95%, and the content of the structural analogue 3α-naveledadine sodium is 0.03%.

Embodiment 2

[0074] 350 grams of naveladine sodium crude product was completely dissolved in 2L of water at 20°C, then 4L of ethyl acetate was added thereto, stirred, and washed with 0.5M H 2 SO 4 Adjust the pH below 4, statically discard the water phase, and then add an ethanol solution containing 1M NaOH to it until the pH is above 800mL, add a total of 800mL of an ethanol solution containing 1M NaOH, collect the precipitate by filtration, and dry it in vacuum to obtain the refined naphthalene Taiding sodium white crystalline powder 330 grams.

[0075] Its assay result and the comparative data with naveladine sodium crude product purity are as follows:

[0076]

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Abstract

The invention discloses a preparation method of sodium salt of pravastatin, which comprises the following steps: adding inorganic alkaline or organic alkaline containing sodium ions as positive ions into organic solution containing the pravastatin until pH is more than 7 and obtaining sodium pravastatin; the organic solution containing the pravastatin comprises the pravastatin and first solvent, wherein the first solvent is selected from one or a plurality of methyl formate, n-propyl formate, isopropyl formate, n-butyl formate, methyl acetate, ethyl acetate, n-propyl acetate, isopropyl acetate, n-butyl acetate, sec-butyl acetate, isobutyl acetate and tert-butyl acetate.

Description

technical field [0001] The present invention relates to the preparation method of the sodium salt of naveladine. Background technique [0002] Naveladine sodium (pravastatin sodium) is one of the statins, its chemical name is {1S-[1α(βs * , δs * ), 2α, 6α, 8β (R * ), 8aα]}-1,2,6,7,8,8a-hexahydro-β,δ,6-trihydroxy-2-methyl-8-(2-methyl-1-oxobutoxy) -1-naphthoyl heptanoic acid monosodium salt, which and lovastatin, simvastatin, atorvastatin, fluvastatin and their derivatives and analogues are hydroxymethylglutaryl coenzyme A (HMG-CoA) Reductase inhibitors are used in the treatment of hypercholesterolemia or atherosclerosis. [0003] [0004] The structural formula of naveladine sodium [0005] Naveladine sodium exerts its lipid-lowering effect from two aspects: first, it reversibly inhibits the activity of HMG-CoA reductase, blocks the biosynthesis of cholesterol in the liver, reduces the amount of cholesterol in cells to a certain extent, stimulates The compensatory in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/013C07C69/22C07C67/48C07C67/28A61K31/22A61P3/06A61P9/10
Inventor 季晓铭姚勇卓忠浩宫鹏飞马宝练褚军锡书毅邢伟
Owner SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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