Name | Quinapril hydrochloride |
Synonyms | Korec ccupril Acupril Korectic Quinazil Quinapril Quinapril hcl Quinapril hydrochloride (3S)-2-[(2S)-2-[[(1S)-1-carbethoxy-3-phenyl-propyl]amino]propanoyl]-3,4-dihydro-1H-isoquinoline-3-carboxylic acid hydrochloride (3S)-2-[(2S)-2-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxylic acid hydrochloride (3S-(2(R*(R*)),3R*))-2-(2-((1-(Ethoxycarbonyl)-3-phenylpropyl)amino)-1-oxopropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxylic acid monohydrochloride |
CAS | 82586-55-8 |
EINECS | 620-479-5 |
InChI | InChI=1/C25H30N2O5.ClH/c1-3-32-25(31)21(14-13-18-9-5-4-6-10-18)26-17(2)23(28)27-16-20-12-8-7-11-19(20)15-22(27)24(29)30;/h4-12,17,21-22,26H,3,13-16H2,1-2H3,(H,29,30);1H/t17-,21-,22-;/m0./s1 |
Molecular Formula | C25H31ClN2O5 |
Molar Mass | 474.98 |
Melting Point | 120-130°C |
Boling Point | 662°C at 760 mmHg |
Specific Rotation(α) | D23 +14.5° (c = 1.2 in ethanol) (Klutchko); D25 +15.4° (c = 2 in methanol) (Goel, Krolls) |
Flash Point | 354.1°C |
Solubility | H2O: >10mg/mL |
Vapor Presure | 2E-18mmHg at 25°C |
Appearance | solid |
Color | white |
Storage Condition | 2-8°C |
Sensitive | Sensitive to light |
MDL | MFCD00889215 |
Use | Used as an antihypertensive agent |
In vitro study | Quinapril (hydrochloride) (CI-906) is an angiotensin-converting enzyme inhibitor (ACE inhibitor) used in the treatment of hypertension and congestive heart failure. Quinapril is rapidly de-esterified after absorption to quinaprilat (the active diacid metabolite), a potent angiotensin converting enzyme (ACE) inhibitor. |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
WGK Germany | 2 |
RTECS | NW7176000 |
HS Code | 2933492250 |
Toxicity | Freely sol in aq solvents. LD50 in male, female mice, rats (mg/kg): 1739, 1840, 4280, 3541 orally; 504, 523, 158, 107 i.v. (Kaplan, 1989) |
This product is (S)-2-[(S)-N-[(S)-l-alkyl-3-phenylpropyl] alanyl]-1,2,3, 4-tetrahydro-3-isoquinoline carboxylic acid -1-ethyl ester hydrochloride. The content of C25H30N2O5. HC1 should be between 98.0% and 102.0% based on the water content.
specific rotation
take this product, precision weighing, add methanol to dissolve and quantitative dilution to make a solution containing about 20mg per lml, according to the law (General 0621), the specific rotation was 13.0 ° to 17.0 °.
take 1.0g of this product, add 1000ml of water to dissolve, and measure according to law (General rule 0631). The pH value should be 2.0~3.0.
take this product about O.lg, precise weighing, in a Erlenmeyer flask, Add 10ml of ethanol and 50ml of water to dissolve, add nitric acid to acidify, according to potentiometric titration (General rule 0701), titration with silver nitrate titrant (0.05mol/L) corresponds to 1.7725mg of C1 per 1 ml of silver nitrate titrant (0.05mol/L). The chloride content shall be 7. 2-7.6% based on chlorine (C1).
operation in the dark. Take an appropriate amount of this product, add water to dissolve and dilute to make a solution containing about 0.5mg per 1ml as a test solution; Take 1ml of the test solution for precision measurement and put it in a 100ml measuring flask, as a control solution, it was diluted to the scale with water and shaken. According to the chromatographic conditions under the content determination item, 20 ml of the test solution and 20 ml of the control solution are respectively injected into the liquid chromatograph, and the chromatogram is recorded to 3 times of the retention time of the main component peak. If there is a chromatographic peak in the chromatogram of the test solution that is consistent with the retention time of impurity I peak, the peak area shall not be greater than the main peak area of the control solution (1.0% ) ; the Peak area of other individual impurities shall not be greater than 0.5 times (0.5%) of the main peak area of the control solution; The sum of the peak areas of other impurities shall not be greater than 1.5 times (1.5%) of the main peak area of the control solution.
take about 0.5g of this product, precision weighing, adding water to dissolve and quantitatively dilute to make a solution containing about 10 mg per lml, take 4ml for precision measurement, place in a top empty bottle, Seal, as a test solution; Take an appropriate amount of acetonitrile, precision weighing, quantitative dilution with water to make about 4 per 1 ml. 4ml of lug solution was precisely weighed, placed in a headspace bottle, and sealed as a reference solution. Test as residual solvent assay (General 0861 first method). Polyethylene glycol 20m (or similar polarity) was used as stationary liquid; Column temperature was 80°C; Inlet temperature was 140°C; Detector temperature was 180°C; Headspace bottle equilibrium temperature was 80°C, the equilibration time was 30 minutes. The test solution and the reference solution were injected by Headspace, and the chromatograms were recorded. According to the external standard method to calculate the peak area, the residual amount of acetonitrile should be in accordance with the provisions.
take this product, according to the moisture determination method (General 0832 first method 1), the water content shall not exceed 1.0%.
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
The residue from taking the item of fulminant fishing shall not contain more than 20 parts per million of heavy metals as inspected by law (General rule 0821, Law II).
operation in the dark. Determined by high performance liquid chromatography (General 0512).
silica gel bonded with eighteen alkyl silane was used as the filler; Methanol-water-diethylamine phosphate (60:40:0.13:0.16) was used as the mobile phase; The detection wavelength was 215nm; The column temperature was 40°C. Take Quinapril Hydrochloride with [3S-[2(R),3a ,llaB]]-l,3,4,6,ll,lla-hexahydro-3-methyl-1, 4-dioxo-a-(2-phenylethyl)-2H-batch of azino [1,2-6] isoquinolin-2-acetic acid ethyl ester (impurity I), water is added to dissolve and dilute to make a solution containing 5ug per 1 ml, and 20 u1 is injected into the liquid chromatograph. The separation degree of Quinapril peak and impurity I peak should be greater than 4.0. The number of theoretical plates is not less than 1000 based on the Quinapril peak.
take this product, precision weighing, add water to dissolve and quantitatively dilute to make a solution containing 0.2mg of Quinapril Hydrochloride per 1 mL (with new preparation), as a test solution, 20 u1 was accurately measured, and human liquid chromatograph was injected to record the chromatogram. Another reference substance of Quinapril Hydrochloride was also accurately weighed and determined by the same method. According to the external standard method to calculate the peak area, that is.
angiotensin-converting enzyme inhibitors.
below 30°C, sealed storage.