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Novel pitavastatin nitryl ester derivant

A technology of pitavastatin and derivatives, which is applied in the field of medicine and achieves the effects of being suitable for long-term application, reducing blood lipids and having a small dosage

Inactive Publication Date: 2008-09-24
BEIJING RUNDEKANG MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, any drug has its duality, that is, therapeutic effect and adverse reaction

Method used

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  • Novel pitavastatin nitryl ester derivant
  • Novel pitavastatin nitryl ester derivant
  • Novel pitavastatin nitryl ester derivant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1 Preparation of pitavastatin 4-(nitrooxy)butyl ester (I1)

[0018] Dissolve 8.9g of pitavastatin sodium in 60ml of DMF, cool in an ice-water bath, and add dropwise 6.5g-30ml of 1,4-dibromobutane in DMF. After dropping, the temperature was raised to room temperature for 22 hours. Concentrate to dryness under reduced pressure, add water and ether, dry the organic phase over anhydrous sodium sulfate and concentrate to dryness. After passing through the column, eluting with petroleum ether: ethyl acetate = 3:1, the desired components were collected and evaporated to dryness under reduced pressure to obtain pitavastatin 4-bromobutyl ester.

[0019] The pitavastatin 4-bromobutyl ester obtained above was dissolved in 100 ml of acetonitrile, 3.4 g of silver nitrate was added, and the reaction was stirred at room temperature in the dark for 48 h. Filtrate, concentrate the filtrate to dryness under reduced pressure, pass through the column, elute with petroleum ether: ...

Embodiment 2

[0020] Example 2 Preparation of pitavastatin 4-(nitrooxymethyl)benzyl ester (I2)

[0021] Dissolve 8.9 g of pitavastatin sodium in 60 ml of DMF, cool in an ice-water bath, and add 7.0 g to 30 ml of p-dichloromethylbenzene in DMF solution dropwise. After dropping, the temperature was raised to room temperature for 24 hours. Concentrate to dryness under reduced pressure, add water and ethyl acetate, dry the organic phase over anhydrous sodium sulfate and concentrate to dryness. After passing through the column and eluting with petroleum ether: ethyl acetate = 1:1, the desired components were collected and evaporated to dryness under reduced pressure to obtain pitavastatin 4-chloromethylbenzyl ester.

[0022] The pitavastatin 4-chloromethylbenzyl ester obtained above was dissolved in 80 ml of acetonitrile, 4.0 g of silver nitrate was added, and the reaction was stirred at room temperature in the dark for 48 h. Filtrate, concentrate the filtrate to dryness under reduced pressure...

Embodiment 3

[0023] Example 3 Preparation of pitavastatin 2-(nitrooxymethyl)benzyl ester (I3)

[0024] Dissolve 8.9 g of pitavastatin sodium in 60 ml of DMF, cool in an ice-water bath, and add 7.0 g to 30 ml of o-dichloromethylbenzene in DMF solution dropwise. After dropping, the temperature was raised to room temperature for 24 hours. Concentrate to dryness under reduced pressure, add water and ethyl acetate, dry the organic phase over anhydrous sodium sulfate and concentrate to dryness. After passing through the column, eluting with petroleum ether: ethyl acetate = 1:1, the desired components were collected and evaporated to dryness under reduced pressure to obtain pitavastatin 2-chloromethylbenzyl ester.

[0025] The pitavastatin 2-chloromethylbenzyl ester obtained above was dissolved in 80 ml of acetonitrile, 3.6 g of silver nitrate was added, and the reaction was stirred at room temperature in the dark for 48 h. Filtrate, concentrate the filtrate to dryness under reduced pressure, p...

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Abstract

The present invention provides novel pitavastatin nitro ester derivative that is shown in the formula (I). The derivative comprises acceptable salt, hydrate or solvolyte in the pharmacy. In the formula (I), X stands for O, S and NH; R has a bivalent group defined as follows: (a) alkyl or substitutional alkyl with 1 to 20 carbon atoms that can be freely substituted by one or more than one substitutional group; or amino group with 3 to 7 carbon atoms that can be substituted by one or more than one substitutional group; (b) amino acid residue containing hydroxyl, such as serine and threonine residue; (c) n standing for an integral from 0 to 20 and m standing for an integral from 0 to 20.

Description

technical field [0001] The invention relates to a novel pitavastatin nitro ester derivative, which belongs to the technical field of medicine. Background technique [0002] Blood lipids are some fats in human blood. These fats are mainly cholesterol and triglycerides. There is another kind called lipids. Lipids here include phospholipids, glycolipids and sterols. These are collectively called blood lipids. . Hyperlipidemia is a disease of systemic metabolic abnormalities caused by various causes of plasma cholesterol, triglycerides, and low-density lipoprotein levels and low high-density lipoprotein levels. It is clinically divided into There are five types I, II, III, IV, and V. Abnormal metabolism in any of the five types will lead to an increase in a specific lipoprotein. By judging which type of lipoprotein is elevated, you can determine which type it is Hyperlipidemia, the most common type II and IV. [0003] The general performance of hyperlipidemia is not very obvi...

Claims

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Application Information

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IPC IPC(8): C07D215/14A61K31/47A61P3/06
Inventor 姚勇敢
Owner BEIJING RUNDEKANG MEDICAL TECH CO LTD
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