Benazepril | 86541-75-5

Benazepril Properties

Melting point	148-149°
alpha	D -159° (c = 1.2 in ethanol)
Boiling point	691.2±55.0 °C(Predicted)
Density	1.26±0.1 g/cm3(Predicted)
storage temp.	2-8°C
solubility	Soluble in DMSO
pka	3.73±0.10(Predicted)
BCS Class	1
CAS DataBase Reference	86541-75-5(CAS DataBase Reference)
FDA UNII	UDM7Q7QWP8
ATC code	C09AA07

SAFETY

Risk and Safety Statements

Safety Statements	22-24/25

Benazepril price

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
TRC	B119858	BenazeprilFreeBase	86541-75-5	2.5g	$1825	2021-12-16	Buy
American Custom Chemicals Corporation	API0001603	BENAZEPRIL 95.00%	86541-75-5	5G	$2607.41	2021-12-16	Buy
ApexBio Technology	B1278	Benazepril	86541-75-5	250mg	$45	2021-12-16	Buy
Medical Isotopes, Inc.	18510	Benazepril	86541-75-5	25mg	$1500	2021-12-16	Buy
ChemScene	CS-1795	Benazepril	86541-75-5	500mg	$80	2021-12-16	Buy

Product number	Packaging	Price	Buy
B119858	2.5g	$1825	Buy
API0001603	5G	$2607.41	Buy
B1278	250mg	$45	Buy
18510	25mg	$1500	Buy
CS-1795	500mg	$80	Buy

Benazepril Chemical Properties,Uses,Production

Originator

Lotensin,Novartis

Uses

Benazepril Free base is a non-sulfhydryl ACE inhibitor.

Definition

ChEBI: A benzazepine that is benazeprilat in which the carboxy group of the 2-amino-4-phenylbutanoic acid moiety has been converted to the corresponding ethyl ester. It is used (generally as its hydrochloride salt) as a prodrug for the angiotensin-converting enzy e inhibitor benazeprilat in the treatment of hypertension and heart failure.

Manufacturing Process

The synthesis of benzazepril based on a benzazepinone. It started by chlorination of lactam - 1,2,4,5-tetrahydrobenzo[b]azepin-2-one to the dichloro derivative 3,3-dichloro-1,2,4,5-tetrahydrobenzo[b]azepin-2-one. Catalytic reduction removed one of the gem chloro substituents to give 3- chloro-1,2,4,5-tetrahydrobenzo[b]azepin-2-one; the halogen was then displaced with sodium azide to give 3-azido-1,3,4,5- tetrahydrobenzo[b]azepin-2-one. Alkylation of the amide with ethyl bromoacetate in the presence of base yielded the ester (3-azido-2-oxo- 2,3,4,5-tetrahydrobenzo[b]azepin-1-yl)acetic acid ethyl ester. Hydrogenation then converted the azide to an amino group to give 3-amino-2-oxo-2,3,4,5- tetrahydrobenzo[b]azepin-1-yl)acetic acid ethyl ester. It was then resolved by classical salt formation and crystallization. Saponification of the S enantiomer - S-(3-amino-2-oxo-2,3,4,5-tetrahydrobenzo[b]azepin-1-yl)acetic acid ethyl ester with sodium hydroxide afforded (3-amino-2-oxo-2,3,4,5- tetrahydrobenzo[b]azepin-1-yl)acetic acid. Reductive alkylation of it with 2- oxo-4-phenylbutyric acid ethyl ester and sodium cyanoborohydride gave the desired product as 70:30 mixture of diastereoisomers. The isolation of the predominant isomer gave benazepril. The epimerization occurred thermally and therefore required a sufficiently high temperature. The high temperature condition can be achieved by either using a high boiling-point solvent such as xylene or by heating the reaction mixture under pressure to increase its boiling-point temperature. Good results can be achieved in both polar and non-polar solvent systems. For example, both p-xylene and ethylene glycolwater systems are found suitable to conduct this process. The crude product acid 3-[(1-ethoxycarbonyl)-3-phenyl-(1S)-propylamino]-2,3,4,5-tetrahydro-2- oxo-1H-1-benzazepine-1-acetic acid was heated to reflux temperature for 30 hours in p-xylene. The mixture was cooled down to room temperature. Solvent removal resulted in a solid, which was then dried at reduced pressure to give a 98:2 diasteriomeric mixture as determined by HPLC, MP: 287°- 290°C. IR and 1H-NMR spectrum analysis. was confirmed the structure of product.

Therapeutic Function

Antihypertensive

Enzyme inhibitor

This ACE-directed pro-drug (FWfree-acid = 424.50 g/mol; CAS 86541-75-5), also known as 3-((1-(ethoxycarbonyl)-3-phenylpropyl)amino)-2,3,4,5- tetrahydro-2-oxo-(S-(R*,R*))-1H-1-benzazepine-1-acetic acid, Lotensin and CGS 14824A, is rapidly metabolized to its diacid benazeprilat (CGS 14831; FWfree-diacid = 396.44 g/mol), the latter a potent, long-acting inhibitor of peptidyl-dipeptidase A, or angiotensin I-converting enzyme, IC50 = 1.7 nM. Lotensin is used to treat hypertension, congestive heart failure, and chronic renal failure. The antihypertensive effects of benazepril begin as early as 30 min after a single dose, and those effects during consecutive dosing are also sustained for 24 h with a lesser diurnal variation in blood pressure

Benazepril synthesis

Synthesis of Benazepril from Benazepril hydrochloride

Benazepril Preparation Products And Raw materials

Raw materials

4-Methylmorpholine Cinchonidine Sulfurous Acid 4-Nitrobenzenesulfonyl chloride Tert-butyl ester

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

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Preparation Products

Benazepril Suppliers

Global( 149)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
Jiangxi Huihe Chemical Co., Ltd.	+86-19189228086 +8618858568638	wuzhouding@huihecrop.com	China	886	58
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Xiamen AmoyChem Co., Ltd	+86-592-6051114 +8618959220845	sales@amoychem.com	China	6387	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58
Alchem Pharmtech,Inc.	8485655694	sales@alchempharmtech.com	United States	63711	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	47465	58
Shandong Hengshannuode Pharmaceutical Technology Co., Ltd.	+8615065888978	admin@hsnordpharma.com	China	92	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
Shaanxi Dideu Medichem Co. Ltd	+86-029-89586680 +86-18192503167	1026@dideu.com	China	9553	58
Hebei Lingding Biotechnology Co., Ltd.	+86-18031140164 +86-19933155420	erin@hbldbiotech.com	China	879	58

Supplier	Advantage
Jiangxi Huihe Chemical Co., Ltd.	58
career henan chemical co	58
Xiamen AmoyChem Co., Ltd	58
Chongqing Chemdad Co., Ltd	58
Alchem Pharmtech,Inc.	58
CONIER CHEM AND PHARMA LIMITED	58
Shandong Hengshannuode Pharmaceutical Technology Co., Ltd.	58
TargetMol Chemicals Inc.	58
Shaanxi Dideu Medichem Co. Ltd	58
Hebei Lingding Biotechnology Co., Ltd.	58

View Lastest Price from Benazepril manufacturers

Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
2023-09-14	Benazepril 86541-75-5	US $0.00-0.00 / g	100g	99%	20 tons	Wuhan Han Sheng New Material Technology Co.，Ltd
2023-04-19	Benazepril 86541-75-5	US $50.00 / kg	1kg	99%	50 tons	Hebei Duling International Trade Co. LTD
2021-11-03	Benazepril 86541-75-5	US $0.00-0.00 / Kg/Drum	1KG	98%min	100kg	WUHAN FORTUNA CHEMICAL CO., LTD

Benazepril
86541-75-5
US $0.00-0.00 / g
99%
Wuhan Han Sheng New Material Technology Co.，Ltd

Benazepril
86541-75-5
US $50.00 / kg
99%
Hebei Duling International Trade Co. LTD

Benazepril
86541-75-5
US $0.00-0.00 / Kg/Drum
98%min
WUHAN FORTUNA CHEMICAL CO., LTD

Benazepril Spectrum

Benazepril(86541-75-5)¹HNMR

86541-75-5(Benazepril)Related Search:

PHENYL VALERATE Phenylhydrazine Glycine 3,4'-DIAMINODIPHENYLMETHANE 1,1'-Carbonyldiimidazole

Propyl gallate Lithium diisopropylamide Propyl butyrate ALTRENOGEST Carbonyl iron powder

S-ATBA Benazepril Related Compound G Benazepril hydrochloride NICKEL CARBONYL Benazepril Related Compound D

Benazepril Related Compound F Hydrocortisone CORTISONE

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2-[(4s)-4-[[(1s)-1-ethoxycarbonyl-3-phenyl-propyl]amino]-5-oxo-6-azabicyclo[5.4.0]undeca-7,9,11-trien-6-yl]acetic acid genazepril BENAZEPRIL HCL, RELATED COMPOUND B(3S)-3-[[(1R)-1-(ETHOXYCARBONYL)-3-PHENYLPROPYL]AMINO]-2,3,4,5-TETRAHYDRO-2-OXO-1H-1-BENAZAPINE-1-ACETIC ACID, MONOHYDROCHLORIDE USP STANDARD BENAZEPRIL HCL, MM(CRM STANDARD) BENAZEPRIL HCL, USP STANDARD BENAZEPRIL HCL USP(CRM STANDARD) BENAZEPRIL MM BENAZEPRIL MM(CRM STANDARD) BENAZEPRIL FREE BASE BENAZCPRIL 1H-1-Benzazepine-1-acetic acid, 3-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-, (3S)- 1H-1-Benzazepine-1-acetic acid, 3-[[1-(ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-, [S-(R*,R*)]- Benapril Briem Cibacen WS Cibacene (3S)-3-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid [S-(R^<*>^，R^<*>^)]-3-[[1- (Ethoxycarbonyl)-3-phenylpropyl]amino]-2，3，4，5-tetrahydro-2-oxo-lH-1-benzazepine-1-acetic acid Cibacene：Lotensin 2-[(4S)-4-[[(1S)-1-ethoxycarbonyl-3-phenyl-propyl]amino]-3-oxo-2-azabicyclo[5.4.0]undeca-7,9,11-trien-2-yl]acetic acid (3S)-3-[[(S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid 2-[(3S)-3-[[(1S)-1-Ethoxycarbonyl-3-phenylpropyl]amino]-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine-1-yl]acetic acid Cibcen WS Benazepril Benazapril 2-[(3S)-3-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]aMino}-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]acetic acid 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 Benazepril USP/EP/BP 2-((S)-3-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-1-yl)acetic acid Bifeprunox Impurity 16 86541-75-5 C24H28N2O5 API Antihypertensive Active Pharmaceutical Ingredients