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Two crystal forms of amide compound, preparation methods and applications thereof
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A technology of amide compounds and crystal forms, which is applied in the two crystal forms, preparation and application fields of amide compounds, can solve problems such as elevated transaminases, liver function damage in patients, and the impact of low-density lipoprotein levels. The effects of stability and good market development prospects
Active Publication Date: 2014-06-04
SHANGHAI INST OF PHARMA IND +1
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Problems solved by technology
However, long-term use of statins (that is, HMG-CoA reductase inhibitors) in addition to digestive system symptoms such as upper abdominal discomfort, a considerable number of patients will cause liver function damage, elevated transaminases, muscle pain, and elevated creatinekinase ;Phenoxyaromatic acid drugs are generally well tolerated, and some patients have some mild gastrointestinal reactions, but these drugs generally have little effect on blood cholesterol and low-density lipoprotein levels
Attempts to combine the two types of drugs have resulted in severe side effects of rhabdomyolysis syndrome in some patients
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Embodiment 1
[0046] Preparation of Form A of 5-(2,5-dimethylphenoxy)-N-(2-(4-hydroxyphenyl)-2-oxoethyl)-2,2-dimethylpentanamide
[0047] Put 1g of 5-(2,5-dimethylphenoxy)-N-(2-(4-hydroxyphenyl)-2-oxoethyl)-2,2 dimethylpentanamide in a stirring In the container, add 20ml of methanol to it at 20°C, start stirring to dissolve the solute at 20°C, concentrate the solution within 4 hours, and check that the obtained solid is 5-(2,5-dimethylbenzene hemihydrate) after drying Form A of oxy)-N-(2-(4-hydroxyphenyl)-2-oxoethyl)-2,2-dimethylpentanamide. Its powderdiffraction spectrum and DSC spectrum are with embodiment 3.
Embodiment 2
[0049] Preparation of Form A of 5-(2,5-dimethylphenoxy)-N-(2-(4-hydroxyphenyl)-2-oxoethyl)-2,2-dimethylpentanamide
Embodiment 3
[0052] Preparation of Form A of 5-(2,5-dimethylphenoxy)-N-(2-(4-hydroxyphenyl)-2-oxoethyl)-2,2-dimethylpentanamide
[0053] Put 3g of 5-(2,5-dimethylphenoxy)-N-(2-(4-hydroxyphenyl)-2-oxoethyl)-2,2 dimethylpentanamide in a stirring In a container, add 45ml of dichloromethane to it at 40°C and start stirring to dissolve the solute at 40°C, cool the solution to 20°C at a rate of 1°C / min, filter the suspension, and test the obtained filter cake after drying. Form A of 5-(2,5-dimethylphenoxy)-N-(2-(4-hydroxyphenyl)-2-oxoethyl)-2,2-dimethylpentanamide.
[0054] In powder X-raydiffraction spectrum using radiation source Cu-Kα, at diffraction angle 2θ=7.62, 8.80, 9.00, 10.34, 10.96, 15.14, 15.61, 15.99, 17.27, 20.63, 21.89, 22.06, 22.44, 24.28, 24.46 , There is a main diffraction peak at 27.04 degrees, the 2θ error range is ±0.2, see the spectrum figure 1 , figure 1 The middle ordinate represents the diffraction intensity (unit 10 3 CPS), the abscissa represents the diffraction a...
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Abstract
The present invention provides two crystal forms of an amide compound, preparation methods and applications thereof. The present invention provides a crystal form A of an amide compound, wherein the crystal form A is a hemihydrate of 5-(2,5-dimethylphenoxy)-N-(2-(4-hydroxyphenyl)-2-oxoethyl)-2,2 dimethyl pentanamide, the crystal belongs to a triclinic system, the space group is P-1, the crystal cell parameters comprise that a is 12.3753(9) angstrom, b is 18.7755(19) angstrom, c is 19.6882(16) angstrom, alpha is 89.558(6) DEG, beta is 87.184(4) DEG and gamma is 70.789(4) DEG, the crystal cell volume V is 4314.5(6) angstrom<3>, and the asymmetric unit number Z in the crystal cell is 2. The present invention further provides a crystal form B of the amide compound, and a preparation method of the crystal form B. According to the present invention, the two crystal forms have good stability and can be used for preparing pharmaceutical preparations.
Description
technical field [0001] The invention relates to two crystal forms of amide compounds, a preparation method and applications thereof. Background technique [0002] Cardiovascular and cerebrovascular diseases are currently the most serious disease that endangers human life and health, and are common and frequently-occurring diseases among middle-aged and elderly people. It ranks first in morbidity and mortality in many countries. Atherosclerosis is the basis of many cardiovascular and cerebrovascular diseases. A large number of experimental and clinical data prove that atherosclerosis is closely related to abnormal blood lipid metabolism. Therefore, lipid-regulating drugs have become an important field of current drug research. [0003] At present, there are many clinical and commonly used drugs for regulating blood lipids, such as HMG-CoA reductase inhibitors, phenoxyaromatic acids, ion exchange resins or bile acid chelating agents, nicotinic acid and other blood lipid regu...
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