The preparation method of rosiglitazone tartrate

A technology of tartrate and diketone, which is applied in the field of preparation of roger tartrate and new thiazolidinedione derivatives, can solve the problems of high price, limited clinical application, high price, etc., achieve short reaction time, good pharmaceutical properties, and fast effect

Active Publication Date: 2015-12-02
KAIFENG PHARMA GRP +1
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the rosiglitazone currently used in China is mostly imported, the price is relatively high, and the price is expensive, which is unbearable for ordinary patients, so that the clinical application is limited.

Method used

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  • The preparation method of rosiglitazone tartrate

Examples

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Embodiment

[0012] Example: Preparation of 5-[4-[2-methyl-N-(2-pyridyl)amino)ethoxy]thiazolidine-2,4-dione tartrate

[0013] Add 12g of 5-[4-[2-methyl-N-(2-pyridyl)amino)ethoxy]thiazolidine-2,4-dione into a 500mL reaction flask, then add 350mL of absolute ethanol and stir Until it is completely dissolved, heat to reflux until the system is clear, add 5.3g of tartaric acid, and continue to reflux and stir for 1h. After the reaction was completed, it was naturally cooled to room temperature, a white solid was precipitated, filtered, washed with absolute ethanol (10mL×3), and the product was air-dried at 60°C under normal pressure for 12h, with a yield of 95%. IR(KBr):3453,3342,3253,3070,2983,2929,2896,2783,1751,1697,1629,1540,1512,1461,1413,1351,1287,1234,1174,1133,1075,941,921,901,838,750,721,673,620,599,556,524,507cm -1 ; 1 HNMR(400MHz,DMSO): δ 12.3(s,2H),8.08(d, J =3.6Hz,1H),7.50(m,1H),7.13(d, J =8.4Hz,2H),6.87(d, J =8.4Hz,2H),6.64(d, J =8.4Hz,1H),6.56(t, J =6.0Hz,1H),5.13(m,1H...

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Abstract

The invention discloses a method for preparing rosiglitazone tartrate, relates to a method for preparing a novel medicinal compound, namely 5-[4-[2-methyl-N-(2-pyridyl) amino] ethoxy] thiazolidine-2,4-diketone tartrate, and belongs to the field of medicinal chemistry. The method comprises the following steps of: adding 5-[4-[2-methyl-N-(2-pyridyl) amino] ethoxy] thiazolidine-2,4-diketone into a polar solvent, adding tartaric acid with heating to dissolve the 5-[4-[2-methyl-N-(2-pyridyl) amino] ethoxy] thiazolidine-2,4-diketone, refluxing, cooling to room temperature after the reaction is finished, filtering, drying, and thus obtaining a product. The method is high in yield, short in reaction time, very simple in post treatment and convenient for industrialized production. The prepared compound can be used for treating type II diabetes and multiple diabetic complications, and is high in bioavailability and quick in response; and the pharmacokinetics of the compound is not affected by age.

Description

technical field [0001] The present invention relates to a kind of preparation method of novel thiazolidinedione derivative, especially relates to tartrate rogergol [0002] The invention discloses a preparation method of ketone, which belongs to the field of medicinal chemistry. Background technique [0003] Diabetes is a common and frequently-occurring disease. The number of patients is increasing rapidly with the changes in people's lifestyles and the aging of the population. Once the disease occurs, it is necessary to take medicine for life; the prevalence, disability and mortality of diabetes And the degree of overall health hazard has ranked third among non-communicable diseases, becoming the third largest disease that seriously threatens human health after cardiovascular and cerebrovascular diseases and tumors. Diabetes can also induce a variety of diseases, seriously endanger people's health and life, and bring a heavy economic burden to society. Therefore, the rese...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D417/12C07C59/255C07C51/41A61P3/10
Inventor 吴亚朱松林朱成功周振陈水库
Owner KAIFENG PHARMA GRP
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