Benazepril hydrochloride

Benazepril hydrochloride Properties

Melting point	188-190°C
alpha	D -141.0° (c = 0.9 in ethanol)
storage temp.	2-8°C
solubility	DMSO: ~34 mg/mL, soluble
form	solid
color	white
Merck	14,1031
InChIKey	VPSRQEHTHIMDQM-FKLPMGAJSA-N
SMILES	C12=CC=CC=C1CC[C@H](N[C@H](C(=O)OCC)CCC1C=CC=CC=1)C(=O)N2CC(=O)O.Cl \|&1:8,10,r\|
CAS DataBase Reference	86541-74-4(CAS DataBase Reference)

SAFETY

Risk and Safety Statements

Symbol(GHS)	GHS08
Signal word	Warning
Hazard statements	H361fd
Precautionary statements	P201-P202-P280-P308+P313-P405-P501
Safety Statements	22-24/25
RIDADR	3077
WGK Germany	2
RTECS	CX7065000
HS Code	29337900

Benazepril hydrochloride price More Price(5)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Sigma-Aldrich(India)	PHR1912	Benazepril hydrochloride Pharmaceutical Secondary Standard; Certified Reference Material	86541-74-4	250MG	₹23739.23	2022-06-14	Buy
Sigma-Aldrich(India)	B0935	Benazepril hydrochloride ≥98% (HPLC), solid	86541-74-4	250MG	₹70200.13	2022-06-14	Buy
Sigma-Aldrich(India)	B0935	Benazepril hydrochloride ≥98% (HPLC), solid	86541-74-4	500MG	₹126100.43	2022-06-14	Buy
TCI Chemicals (India)	B3611	Benazepril Hydrochloride	86541-74-4	1G	₹4700	2022-05-26	Buy
TCI Chemicals (India)	B3611	Benazepril Hydrochloride	86541-74-4	5G	₹10000	2022-05-26	Buy

Product number	Packaging	Price	Buy
PHR1912	250MG	₹23739.23	Buy
B0935	250MG	₹70200.13	Buy
B0935	500MG	₹126100.43	Buy
B3611	1G	₹4700	Buy
B3611	5G	₹10000	Buy

Benazepril hydrochloride Chemical Properties,Uses,Production

Description

Benazepril hydrochloride is a long-acting and effective angiotensin-converting enzyme (ACE) inhibitor used to treat essential hypertension. It is the hydrochloride salt form of benazepril, which is a prodrug of benazeprilat. After hepatic cleavage of the ester group, benazepril is converted to benazeprilat. In healthy humans, it was well tolerated and showed no phmacokinetic interactions with furosemide, hydrochlorothiazide, chlorthalidone, digoxin, cimetidine, atenolol, or naproxen.

Chemical Properties

This substance is a white to off-white crystalline powder. It is highly soluble in water, ethanol, and methanol with a solubility of over 100 mg/mL.

Uses

Benazepril HCl is an angiotensin-converting enzyme (ACE) inhibitors that is commonly used as a sedative, hypnotic, and antihypertensive medication. Benazepril is used alone or together with other medicines to treat high blood pressure (hypertension). It works by reducing the levels of certain chemicals that cause blood vessels to constrict, allowing for smoother blood flow.

Definition

ChEBI: Benazepril hydrochloride is a hydrochloride salt resulting from the reaction of benazepril with 1 mol eq. of hydrogen chloride. It is used as a prodrug for angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure. It has a role as an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor. It contains a benazepril(1+).

General Description

Benazepril is a prodrug of the angiotensin converting enzyme (ACE) inhibitor benazeprilat . It is metabolized to benazeprilat by hepatic esterases. Benazepril inhibits the in vitro enzymatic activity of partially purified ACE isolated from rabbit lung (IC50 = 2 nM). It decreases the triglyceride and total cholesterol levels in normotensive rats when administered at a dose of 30 mg/kg and decreases aortic atherosclerosis in cholesterol-fed rabbits when administered at a dose of 3 mg/kg per day. Benazepril (0.1-10 mg/kg per day) reduces blood pressure in spontaneously hypertensive rats. It also decreases proteinuria in cats with chronic kidney disease when administered at doses ranging from 0.5 to 1 mg/kg per day. Formulations containing benazepril have been used to treat hypertension, congestive heart failure, and chronic kidney disease in both human and veterinary medicine.

Biological Activity

Non-peptide angiotensin-converting enzyme (ACE) inhibitor. Reduces blood pressure and myocardial hypertrophy in spontaneous hypertensive rats.

Synthesis

Benazepril hydrochloride is prepared through the following steps:
Step 1: Preparation of (R)-ethyl 2-hydroxy-4-phenylbutyrate using ethyl 2-oxo-4-phenylbutyrate as a raw material and cinchonidine as a chiral ligand through asymmetric catalytic hydrogenation under high pressure.
Step 2: The intermediate obtained from step 1 reacts with p-nitrobenzenesulfonyl chloride or trifluoromethanesulfonic anhydride to obtain the corresponding sulfonate.
Step 3: The sulfonate obtained from step 2 undergoes nucleophilic substitution and salt hydrolysis with (3S)-3-amino-2,3,4,5-tetrahydro-2-oxo-1H-benzazepine-1-tert-butyl acetate to obtain benazepril hydrochloride.
This procedure has been described in detail in documents such as CN110835319A, US4785089, WO02076375, EP206993, and CN105061312.

Mode of action

The mechanism of action of benazepril is to inhibit the activity of the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II Label, thereby alleviating a series of symptoms caused by angiotensin (elevated blood pressure, increased excitatory heart rate caused by vasodilation, insufficient cardiac output, etc.).

References

https://www.novartis.com/us-en/sites/novartis_us/files/lotrel.pdf
https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a216253b-27cb-42ef-b5a8-67fb05aafb88
Extrapyramidal side effect of donepezil hydrochloride in an elderly patient DOI: 10.1097/MD.0000000000019443
Use of convertible isocyanides for the synthesis of benazepril hydrochloride DOI: 10.1007/s12039-021-01892-8

Benazepril hydrochloride Preparation Products And Raw materials

Raw materials

Sodium cyanoborohydride Ethyl 2-oxo-4-phenylbutyrate Sodium azide

Preparation Products

Benazepril

Benazepril hydrochloride Suppliers

Global( 419)Suppliers

Supplier	Tel	Country	ProdList	Advantage	Inquiry
Hetero Drugs Limited	+91-4023704923 +91-4023704923	Telangana, India	296	58	Inquiry
Aarti Industries Limited (AIL)	+91-84596144931 +91-9920899935	Maharashtra, India	235	58	Inquiry
Nuray Chemicals Pvt Ltd	+91-4066616700 +91-8220444745	Tamil Nadu, India	49	58	Inquiry
Sun Pharmaceutical Industries Ltd	+91-2242244224 +91-2243244324	Maharashtra, India	108	58	Inquiry
Aruvi Labs	+91-8056181939 +91-8056181939	Tamil Nadu, India	149	58	Inquiry
Ralington Pharma	+91-7948911722 +91-9687771722	Gujarat, India	1350	58	Inquiry
BDR Pharmaceuticals International Pvt Ltd	+91-2240560560 +91-7718884418	Maharashtra, India	206	58	Inquiry
Unimark Remedies Ltd	+91-2267304120 +91-2267304120	Maharashtra, India	48	58	Inquiry
Molsyns Research	+91-9586858886 +91-9586858886	Gujarat, India	418	58	Inquiry
Synthink Research Chemicals	09158051123	Pune, India	398	58	Inquiry

Supplier	Advantage
Hetero Drugs Limited	58
Aarti Industries Limited (AIL)	58
Nuray Chemicals Pvt Ltd	58
Sun Pharmaceutical Industries Ltd	58
Aruvi Labs	58
Ralington Pharma	58
BDR Pharmaceuticals International Pvt Ltd	58
Unimark Remedies Ltd	58
Molsyns Research	58
Synthink Research Chemicals	58

Benazepril hydrochloride Spectrum

Benazepril hydrochloride(86541-74-4)¹HNMR

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1h-1-benzazepine-1-aceticacid,2,3,4,5-tetrahydro-3-((1-(ethoxycarbonyl)-3-phe cgs14824a monohydrochloride,(s-(r*,r*))-nylpropyl)amino)-2-oxo BenazeprilHclC24H28N205.HC1 1H-1-Benzazepine-1-acetic acid, 3-(1S)-1-(ethoxycarbonyl)-3-phenylpropylamino-2,3,4,5-tetrahydro-2-oxo-, monohydrochloride, (3S)- 1H-1-Benzazepine-1-acetic acid, 3-[[1-(ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-, monohydrochloride, [S-(R*,R*)]- CGS 14824A HCl Lotension Benazenprilhydrochloride {(3S)-3-[(1S)-1-Ethoxycarbonyl-3-phenylpropylamino]-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepin-1-yl}acetic acid hydrochloride Benazepril hydrochloride Benazepril hydrochloride (3S)-3-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid hydrochloride Benazepril Hydrochloride, SS-form 1H-1-Benzazepine-1-acetic acid, 2,3,4,5-tetrahydro-3-((1-(ethoxycarbonyl)-3-phenylpropyl)amino)-2-oxo-, monohydrochloride, (S-(R*,R*))- Cibace Cibacen chf Benazepril hydrochloride,(3S)-3-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid hydrochloride Benazepril Hydrochloride (125 mg) 2-((S)-3-((S)-1-ethoxy-1-oxo-4-phenylbutan-2-ylamino)-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-1-yl)aceticacidhydrochloride Benazepri hydrochloride Benazepril HCl API 1H-1-Benzazepine-1-acetic acid, 3-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]aMino]-2,3,4,5-tetrahydro-2-oxo-, hydrochloride (1:1), (3S)- 2-((S)-3-((S)-1-ethoxy-1-oxo-4-phenylbutan-2-ylamino)-2-oxo-2,3,4,5-tetrahydrobenzo[b]azepin-1-yl)acetic acid hydrochloride Benazepril hydrochloride Benazepril hydrochloride, 98.5%, an angiotensin-converting enzyme (ACE) inhibitor Benazepril Benazepril HCL yansuanbeinapuli 2-[(3S)-3-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]-2-oxo-4,5-dihydro-3H-1-benzazepin-1-yl]acetic acid hydrochloride Benazepril for system suitability CRS BenazeprilHydrochloride> Benazepril hydrochloride CRS Benazepril hydrochloride USP/EP/BP Benazepril HCl （CGS14824A) Benazepril HydrochlorideQ: What is Benazepril Hydrochloride Q: What is the CAS Number of Benazepril Hydrochloride Q: What is the storage condition of Benazepril Hydrochloride Q: What are the applications of Benazepril Hydrochloride Benazepril Hydrochloride (1048619) 3-Cresotic acid Lotensin Benazeprilhydrochloride/CGS14824A Benazepril HCl Reference Standard Benazepril HCI Belapril hydrochloride 86541-74-4 C24H28N2O5HClC24H29ClN2 C24H28N2O5ClH C24H28N2O5HClC24H29ClN2O5 C24H29ClN2O5 SONATA API Amines Aromatics Heterocycles Intermediates & Fine Chemicals Pharmaceuticals 86541-74-4