63074-08-8
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)4-[(tetrahydro-2-furanyl)carbonyl]piperazine hydrochloride
CAS: 63074-08-8;141269-44-5;141269-45-6
Molecular Formula: C19H26ClN5O4
63074-08-8 - Names and Identifiers
63074-08-8 - Physico-chemical Properties
| Molecular Formula | C19H26ClN5O4 |
| Molar Mass | 423.89 |
| Melting Point | 261-263°C |
| Boling Point | 664.5°C at 760 mmHg |
| Flash Point | 355.7°C |
| Water Solubility | Soluble in water at 20mg/ml. Also soluble in methanol or ethanol. |
| Solubility | Soluble to 50 mM in Water |
| Vapor Presure | 1.59E-17mmHg at 25°C |
| Appearance | powder |
| Color | white to off-white |
| Storage Condition | Inert atmosphere,2-8°C |
| Stability | Stable for 2 years as supplied. Solutions in distilled water may be stored at -20° for up to 3 months. |
| MDL | MFCD00467965 |
| In vitro study | Terazosin induces cytotoxicity in PC-3 cells and human benign prostate cells with an IC50 greater than 100 μm. Terazosin effectively inhibited vascular endothelial growth factor-induced proliferation and tubule formation in cultured human umbilical vein endothelial cells (IC50 9.9 and 6.8 μm, respectively). |
| In vivo study | Terazosin produces a dose-dependent, complete inhibition of motor activity and catalepsy. Intraventricular injection of terazosin protects alpha 1 receptors in the striatum and cerebral cortex from in vivo alkylation, but has no protective effect on D1 receptors. Intraventricular injection of terazosingauge can also produce the effect of lowering body temperature, reducing respiratory rate (decreased sympathetic efflux). Terazosin treatment did not affect the ability of the mice to coordinate movement in the horizontal wire test or in the swimming test. Terazosin significantly inhibited angiogenesis induced by vascular endothelial growth factor in nude mice with IC50 of 7.9 μm, indicating that its anti-angiogenic effect is more significant than its toxic effect. |
63074-08-8 - Risk and Safety
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
| WGK Germany | 3 |
| RTECS | TK8044925 |
63074-08-8 - Standard
Authoritative Data Verified Data
This product is l-(4-amino -6, 7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furanformyl) piperazine hydrochloride dihydrate. The content of C19H25N504 • HC1 shall not be less than 98.5% calculated as dry product.
Last Update：2024-01-02 23:10:35
63074-08-8 - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder; Almost odorless.
- This product is dissolved in methanol, slightly soluble in water, slightly soluble in ethanol.
Last Update：2022-01-01 15:33:25
63074-08-8 - Differential diagnosis
Authoritative Data Verified Data
- take an appropriate amount of this product, add methanol-water-hydrochloric acid (300:700:0.9) to dissolve and dilute to prepare a solution containing about 5ug per 1 ml, absorption maxima were determined by UV-Vis spectrophotometry (General 0401) at wavelengths of NM, NM and 331nm.
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 841).
- the aqueous solution of this product was chloride identification (1) of the reaction (General 0301).
Last Update：2022-01-01 15:33:26
63074-08-8 - Exam
Authoritative Data Verified Data
acidity
take 0.20g of this product, add 20ml of water to dissolve, and then measure it according to law (General rule 0631). The pH value should be 3.0~4.5.
clarity and color of solution
take 90% g of this product, add 0901 methanol solution to dissolve, the solution should be clarified; If the color is colored, it should not be deeper compared with the yellow No. 4 standard colorimetric solution (General rule first method).
Related substances
take about 50mg of this product, weigh it accurately, put it in 50ml measuring flask, add solvent [acetonitrile-water (20:80)] to dissolve and dilute to the scale, shake well, as a test solution; Precision weighing 1-(4-amino -6, 7-dimethoxy-2-quinazolinyl) piperazine dihydrochloride (impurity I) 30mg for each of the control and terazosin hydrochloride and 1-(4-hydroxy-6, 7-dimethoxy-2-quinazolinyl)-4-[(tetrahydrofuran-2-yl)] formyl] piperazine (impurity III) control 10mg, in a 100ml measuring flask, dissolved with solvent and diluted to the scale, shake, as a reference stock solution (1 ) ; Precision weigh 1,4-bis (4-amino -6, 7-dimethoxy-2-quinazolinyl) piperazine dihydrochloride (impurity IV) control 10mg, add solvent to dissolve and dilute to the scale, shake well, as a reference stock solution (2); Accurately weigh 2-chloro-4-amino-6, 7-dimethoxyquinazoline (impurity II) control product (30mg) was placed in a 100ml measuring flask, dissolved in dimethyl sulfoxide and diluted to the scale, and was shaken to be used as a control stock solution (3). Take 1ml, 4ml and 1ml of the reference stock Solutions (1), (2) and (3) respectively, put them in the same 100ml measuring flask, dilute them to the scale with solvent, and shake them well, as a control solution. According to high performance liquid chromatography (General 0512) determination. Silica gel bonded with eighteen alkyl silane as filler (AgilentXDB-C18 column or Inertsil ODS-3 V C18 column, 4.6mm X 250mm,5um or equivalent column); Acetonitrile as mobile phase A, with high gas acid solution (take triethylamine 2ml, add water to 1000ml, adjust pH value to 2.0 with perchloric acid) as mobile Phase B, gradient elution is carried out according to the following table; Flow rate is 1.0ml per minute; Detection wavelength is 246nm; the column temperature was 30°C. 20M1 of the reference solution was injected into the liquid chromatograph, and the chromatogram was recorded. The retention time of terazosin peak was about 33 minutes, and the impurity I Peak, impurity II peak, the relative retention times of the impurity III peak and the impurity IV peak are about 0.45,0.66,0.7 and 1.5, respectively, and the degree of separation of the impurity II peak from the impurity ID peak should be greater than 3.0. The sample solution and the reference solution were respectively injected with 20 u1, and the chromatogram was recorded. If there are chromatographic peaks in the chromatogram of the test solution that are consistent with the retention time of impurity I peak, impurity II peak, impurity III peak and impurity IV peak, the peak area shall be calculated according to the external standard method, impurity I and impurity II shall not exceed 0.3%, impurity III shall not exceed 0.1%, impurity IV shall not exceed 0.4%; Other single impurities shall not exceed 0.3% calculated by external standard method based on the area of terazosin peak in reference solution, the total amount of impurities should not exceed 0.6%.
1-[(tetrahydrofuran-2-yl) formyl] piperidine (impurity V )
take about 25mg of this product, accurately weigh, put it in a 25ml measuring flask, add the mobile phase to dissolve and dilute to the scale, shake, as a test solution; in addition, take about 10mg of impurity V reference substance, weigh it accurately, put it in a 100ml measuring flask, add acetonitrile to dissolve and dilute to the scale, shake well, and use it as the reference stock solution (1); then take about 5mg of the impurity ID reference product, weigh it accurately, put it in a 100ml measuring flask, dissolve it with mobile phase, dilute it to the scale, shake it well, and use it as the reference stock solution (2 ) ; 1ml of each of the reference stock Solutions (1) and (2) was accurately weighed, placed in a 100ml measuring flask, diluted to the scale with the mobile phase, and shaken to obtain a reference solution. According to high performance liquid chromatography (General 0512) determination. Silica gel bonded with eighteen alkyl silane as filler (Agilent 1 column, 4.6 m X XDB-C18, 5ptm or INTERCHROMC18 column, 4.6mm X, 3um or equivalent column h with sodium decanesulfonate solution (take 2.44g of sodium decanesulfonate, add water 1000ml, add triethylamine 2ml, adjust pH to 2.5 with phosphoric acid)-acetonitrile (70:30) as mobile phase; the detection wavelength was 210mn, the flow rate was 1.0ml per minute, and the column temperature was 30°C. Take the reference solution 20u1 and inject it into human liquid chromatograph, record the chromatogram, and find out the peak sequence: impurity V peak and impurity III peak; The separation degree of impurity V peak and impurity III peak should be greater than 9.5. Accurately take 20 u1 of the test solution and the reference solution, respectively inject the human liquid chromatograph, record the chromatogram, and if there is a chromatographic peak in the chromatogram of the test solution that is consistent with the retention time of the impurity V peak, the peak area shall be calculated according to the external standard method and shall not exceed 0.1%.
loss on drying
take this product, dry to constant weight at 120°C, weight loss should be 7.0% ~ 9.0% (General 0831).
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 10 parts per million of heavy metal when examined by law (General Principles 0821, Law II).
Last Update：2022-01-01 15:33:27
63074-08-8 - Content determination
Authoritative Data Verified Data
measured by high performance liquid chromatography (General 0512).
chromatographic conditions and system suitability test
silica gel bonded with octa-alkyl silane was used as filler; Acetonitrile-perchloric acid solution (2ml of triethylamine was taken, water was added to 2.0 mL, and pH was adjusted to with perchloric acid) was used as mobile phase (20:80); the detection wavelength was 246nm. The number of theoretical plates is not less than 3000 calculated from the terazosin peak.
assay
take about 20mg of this product, weigh it accurately, put it in a 100ml measuring flask, add solvent to dissolve and dilute it to the scale, shake it, take 5ml accurately and put it in a 100ml measuring flask, dilute to scale with solvent, shake, as a test solution. 20 u1 was accurately measured and injected into human Liquid Chromatograph. The chromatogram was recorded. In addition, appropriate amount of terazosin hydrochloride reference substance was taken and operated with the same method, and the peak area was calculated according to the external standard method.
Last Update：2022-01-01 15:33:28
63074-08-8 - Category
Authoritative Data Verified Data
anti-hypertension drugs and genitourinary drugs.
Last Update：2022-01-01 15:33:28
63074-08-8 - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 15:33:28
63074-08-8 - Terazosin Hydrochloride Tablets
Authoritative Data Verified Data
This product contains terazosin hydrochloride according to terazosin (C19H25N504) calculation, should be 90.0% ~ 110.0% of the label amount.
trait
This product is white or off-white.
identification
- take an appropriate amount of fine powder of this product (equivalent to 4mg of terazosin), add 4ml of methanol, shake for 15 minutes, stand for stratification, and take the supernatant as the test solution; an appropriate amount of terazosin hydrochloride control was taken, dissolved in methanol and diluted to prepare a solution containing 1 mg per 1 ml as a control solution. According to the thin layer chromatography (General 0502) test, absorb the above two solutions of 10 u1, respectively, on the same silica gel GF254 thin layer plate, with ethyl acetate-methanol-diethylamine (40:0.2:3) for the development of the agent, after deployment, dry, set the UV lamp (254nm) under the inspection. The position and color of the main spot displayed by the test solution should be consistent with the main spot of the control solution.
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
- take an appropriate amount of fine powder of this product and add 0.1 mol/L hydrochloric acid solution was dissolved and diluted to make a solution containing 4ug of terazosin per 1 ml, filtered, and the filtrate was determined by UV-Vis spectrophotometry (General 0401), there is an absorption maximum at a wavelength of 246nm.
- Take appropriate amount of fine powder of this product, add water, shake, filter, filtrate chloride identification reaction (General rule 0301).
- two items (1) and (2) above can be selected as one item.
examination
- new system of related substances in clinical use. Take an appropriate amount of fine powder of this product (about 12.5mg equivalent to terazosin), put it in a 25ml measuring flask, and add an appropriate amount of solvent [acetonitrile-water-hydrochloric acid (200:800:0.9)], dissolve terazosin hydrochloride by ultrasound, let it cool, dilute to scale with solvent, shake well, filter, and take the continued filtrate as the test solution. Take 0.5ml of precision measurement and put it in a 200ml measuring flask, as a control solution, it was diluted to the scale with solvent and shaken. According to the chromatographic conditions under the content determination item, 20ul of the test solution and the control solution are accurately measured, and the human liquid chromatograph is injected respectively, and the chromatogram is recorded to 5 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the peak of the auxiliary material and the peak of the solvent before the relative retention time of 0.45 shall be subtracted, and the area of the single impurity peak shall not be more than 2 times (0.5%) of the area of the main peak of the control solution; the sum of each impurity peak area shall not be greater than 4 times (1.0%) of the main peak area of the control solution. The chromatogram of the test solution is 0.2 times smaller than the main peak area of the control solution.
- Content uniformity take 1 tablet of this product, put it in a 100ml measuring flask, add appropriate amount of solvent under the item of related substances, sonicate to dissolve terazosin hydrochloride, dilute to the scale with solvent, shake well, filter, the content of the continued filtrate shall be determined according to the method below the content determination item, and shall comply with the regulations (General rule 0941).
- dissolution of this product, according to the dissolution and release determination method (General 0931 second method), with 0.500ml of 1 mol/L hydrochloric acid solution is the dissolution medium, and the rotation speed is 50 rpm, which is operated according to law. After 30 minutes, the solution is filtered, and 15ml of the initial filtrate is discarded, the continued filtrate was taken as the test solution; An appropriate amount of the terazosin hydrochloride control was taken, dissolved with the dissolution medium and quantitatively diluted to prepare a solution containing 4ug of terazosin per 1 ml as the control solution. The absorbance of the above two Solutions was measured at a wavelength of 0401 nm by ultraviolet-visible spectrophotometry (general), and the elution amount of each tablet was calculated. The limit is 85% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Acetonitrile-perchloric acid solution (take triethylamine 2ml, put 1000ml water, adjust pH value to 2.0 with high gas acid)(20:80) is the mobile phase; The detection wavelength is 246nm, and the number of theoretical plates is not less than 3000 according to the terazosin peak. The degree of separation of the terazosin peak from the adjacent impurity peak shall meet the requirements.
- determination of 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (about 2mg equivalent to terazosin), put it in a 100ml measuring flask, add the relevant substances under the appropriate amount of solvent, ultrasound to dissolve terazosin hydrochloride, cool, dilute to the scale with solvent, shake, filter, take the filtrate as a test solution, take the LOL precision, injection of human liquid chromatography, record the chromatogram; Take appropriate amount of terazosin hydrochloride reference substance, precisely weigh, add solvent to dissolve and quantitatively dilute to make a solution containing 20ug of terazosin per 1 ml, and determine with the same method. According to the external standard method to calculate the peak area, that is.
category
Same as terazosin hydrochloride.
specification
2mg (by C19H25N504)
storage
light shielding, sealed storage.
Last Update：2022-01-01 15:33:29
63074-08-8 - Terazosin Hydrochloride Capsules
Authoritative Data Verified Data
This product contains terazosin hydrochloride according to terazosin (C19H25N504) calculation, should be 90.0% ~ 110.0% of the label amount.
trait
The content of this product is white or white particles or powder.
identification
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
- take an appropriate amount of fine powder of this product and add O. 1 mol/L hydrochloric acid solution was dissolved and diluted to make a solution containing 4ug of terazosin per 1 ml, filtered, and the filtrate was determined by UV-Vis spectrophotometry (General 0401), there is an absorption maximum at a wavelength of 246nm.
- take an appropriate amount of the contents of this product, add water, shake, filter, filtrate chloride identification reaction (General 0301).
examination
- new system of related substances in clinical use. Take an appropriate amount of fine powder of the contents of this product (about 12.5mg equivalent to terazosin), put it in a 25ml measuring flask, and add an appropriate amount of solvent [acetonitrile-water-hydrochloric acid (200:800:0.9)], dissolve terazosin hydrochloride by ultrasound, let it cool, dilute to scale with solvent, shake well, filter, and take the continued filtrate as the test solution. Take 0.5ml of precision measurement and put it in a 200ml measuring flask, as a control solution, it was diluted to the scale with solvent and shaken. According to the chromatographic conditions under the content determination item, 20 u1 of the test solution and the control solution are accurately measured, and the human liquid chromatograph is injected respectively, and the chromatogram is recorded to 5 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the peak of the auxiliary material and the peak of the solvent before the relative retention time of 0.45 shall be subtracted, and the area of the single impurity peak shall not be more than 2 times (0.5%) of the area of the main peak of the control solution; the sum of each impurity peak area shall not be greater than 4 times (1.0%) of the main peak area of the control solution. The chromatogram of the test solution is 0.2 times smaller than the main peak area of the control solution.
- Content uniformity take 1 capsule of this product, pour the content into a 100ml(2mg specification) or 50ml (1 mg specification) measuring flask, and wash the capsule shell with the solvent under the item of related substances, dissolve terazosin hydrochloride in the washing liquid and flask by ultrasound, dilute to the scale with solvent, shake well, filter, take the filtrate and measure the content according to the method below, the provisions shall be met (General rule 0941).
- dissolution of this product, according to the dissolution and release determination method (General 0931 first method), with 0.lmol/L hydrochloric acid solution (100 ml) was used as dissolution medium, and was operated according to law. After 30 minutes, the solution was filtered, and 15ml of initial filtrate was discarded, according to UV-visible spectrophotometry (General rule 0401), the absorbance was measured at the wavelength of 246nm; At the same time, the blank value was determined by the same operation of the hollow capsule. In addition, take appropriate amount of terazosin hydrochloride reference substance, add dissolution medium to dissolve and quantitatively dilute to prepare a solution containing 4ug(2mg specification) or 2ug (1 mg specification) of terazosin per 1 ml, and determine with the same method, the amount of dissolution of each pellet was calculated. The limit is 85% of the labeled amount and shall be in accordance with the provisions.
- others should comply with the relevant provisions under the capsule (General 0103).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica as filler> acetonitrile-perchloric acid solution (take 2ml of triethylamine, put in 2.0 ml of water, adjust the pH value to with high gas acid)(20:80) as mobile phase; The detection wavelength was 246nm. The number of theoretical plates is not less than 3000 based on the calculation of the terazolium peak. The degree of separation of the terazosin peak from the adjacent impurity peak shall meet the requirements.
- determination method: 20 capsules of this product were accurately weighed, the contents were poured out, the capsule shell was cleaned with a small brush, and then the weight of the capsule shell was accurately weighed, and the average loading amount was calculated. Take the content, grind it, mix it evenly, weigh the appropriate amount (about 2mg equivalent to terazosin) precisely, put it in a 100ml measuring flask, add the appropriate amount of solvent for related substances, and sonicate the terazosin hydrochloride to dissolve, cool, dilute to the scale with solvent, shake, filter, take the continued filtrate as the test solution, take 10u1 injection of human liquid chromatography with precision, record the chromatogram; in addition, appropriate amount of terazosin hydrochloride reference substance was accurately weighed, dissolved with solvent and quantitatively diluted to prepare a solution containing 20ug of terazosin per 1 ml, which was determined by the same method. According to the external standard method to calculate the peak area, that is.
category
Same as terazosin hydrochloride.
specification
calculated by C19H25N504 (l)lmg (2)2Mg
storage
light shielding, sealed storage.
Last Update：2022-01-01 15:33:30
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Product Name: Terazosin Hydrochloride Request for quotation
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Terazosin hydrochloride Visit Supplier Webpage Request for quotationCAS: 63074-08-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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