Benazepril hydrochloride
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Benazepril hydrochloride
structure -
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CAS No:
86541-74-4
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Formula:
C24H28N2O5.ClH
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Chemical Name:
Benazepril hydrochloride
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Synonyms:
1H-1-Benzazepine-1-acetic acid,3-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-,hydrochloride (1:1),(3S)-;1H-1-Benzazepine-1-acetic acid,3-[[1-(ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-,monohydrochloride,[S-(R*,R*)]-;1H-1-Benzazepine-1-acetic acid,3-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-,monohydrochloride,(3S)-;Benazepril hydrochloride;CGS 14824A;Lotensin;Lotension;CGS 14824A HCl;211307-81-2
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Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs
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CAS No:
Description
Benazepril hydrochloride, an angiotensin converting enzyme inhibitor, which is a medication used to treat high blood pressure.Target: angiotensin converting enzyme (ACE)Benazepril hydrochloride is a medication used to treat high blood pressure (hypertension), congestive heart failure, and chronic renal failure. Upon cleavage of its ester group by the liver, benazepril hydrochloride is converted into its active form benazeprilat, a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibi
Characteristics
95.9
3.83100
white solid
188-190 °C
691.2ºC at 760 mmHg
371.8ºC
DMSO: ~34 mg/mL, soluble
Desiccate at +4°C
D -141.0° (c = 0.9 in ethanol)
Benazepril hydrochloride Use and Manufacturing
Preparation of Highly Pure Benazepril Hydrochloride Through a solution of t-butyl ester of Formula VI in ethyl acetate cooled to about 10 to 12°C was purged dry hydrogen chloride gas slowly without allowing the temperature to rise. The salt formation was monitored by TLC and after completion of the reaction, excess hydrogen chloride and solvent was completely removed under vacuum. To the residue was added, 45 ml acetone and the resultant mixture was stirred for 1 hour at 5-8°C. The product was filtered and dried to constant weight under vacuum at 45-50°C affording 8.27 gm of almost white product with a diastereoisomer ratio of SS: SR = 99. 36: 0. 18. Yield 91.6percent.The feed was heated to reflux and the ethyl acetate was distilled off at atmospheric pressure until the remaining feed solution had a volume of about 500 ml.Cooled to below 10° C , hydrogen chloride gas was bubbled until the absorption saturation, precipitation of solid.Filtered by suction, the filter cake was washed with an appropriate amount of recovered ethyl acetate.The resulting wet crude was added to 500 ml of ethyl acetate and heated to 75 ° C for 4 h.Slowly cool to about 10 ° C, filter, wash the filter cake with appropriate amount of ethyl acetate.After drying under vacuum at 60 ° C, the white benazepril hydrochloride product is about 114g, yield 72percent. The HPLC purity was 99.5percent.
Used as an antihypertensive; angiotensin converting enzyme inhibitor. This product is used for hypertension and congestive heart failure
Drug Function and Efficacy
Extract from the above information
Registered Holders
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NURAY CHEMICALS PRIVATE LTD
Active
United States
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EMCURE PHARMACEUTICALS LTD
Active
United States
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AARTI PHARMALABS LTD
Active
United States
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