cas 86541-74-4, Benazepril hydrochloride | Articles data

Articles about 86541-74-4Total 13 be found

Use of convertible isocyanides for the synthesis of benazepril hydrochloride
Herein, we have described a novel and concise synthesis of the potent angiotensin-converting enzyme (ACE) inhibitor, benazepril hydrochloride (7) in trifluoroethanol via an Ugi three-component reaction in shorter reaction times. The key step is the trifluoroacetic acid-mediated hydrolysis of secondary amides (4a and 4b) followed by esterification as a domino process to form corresponding ethyl ester (6). Mainly two universal convertible isocyanides (1a and 1b) were used for the synthesis of benazepril hydrochloride. Graphic abstract: [Figure not available: see fulltext.] Synopsis: An efficient synthesis of benazepril hydrochloride using Ugi three-component reaction.
Borase, Bhushan B,Godbole, Himanshu M,Singh, Girij P,Upadhyay, Pritesh R,Trivedi, Anurag,Bhat, Varadaraj,Shenoy, Gautham G
(2021/04/19)

Synthesis method of benazepril intermediate and benazepril hydrochloride
The invention relates to a synthesis method of a benazepril intermediate and a benazepril hydrochloride. The synthesis method comprises: carrying out a reaction on 3-bromo-2,3,4,5-tetrahydro-1H-[1]-benzoazepine-2-keto-1-tert-butyl acetate and (S)-homophenylalanine, and carrying out dynamic kinetic resolution to obtain a benazepril intermediate; and carrying out an esterification reaction, and introducing hydrogen chloride gas to obtain a benazepril hydrochloride refined product. According to the invention, the benazepril hydrochloride is efficiently prepared by utilizing a dynamic kinetic resolution technology, so the steps are short, the operation is simple, the total yield is high, the atom economy is high, the environmental pollution is small, and the method is suitable for industrial production.
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Paragraph 0076; 0078-0079; 0081

(2020/03/13)

An improved method for preparing of the benazepril hydrochloride and containing the pharmaceutical composition of the benazepril hydrochloride
The invention discloses an improved preparation method of benazepril hydrochloride and pharmaceutical composition containing the benazepril hydrochloride. With the adoption of the preparation method, the safety is high, the cost is low, the clean production value is high, industrial production is easy to realize, and meanwhile, the pharmaceutical composition is easy to prepare and use.
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Paragraph 0031; 0034; 0038

(2018/01/05)

COMPOSITIONS AND METHODS FOR DIAGNOSING AND TREATING SALT SENSITIVITY OF BLOOD PRESSURE
To characterize the urinary exosome miRNome, microarrays were used to identify the miRNA spectrum present within urinary exosomes from ten individuals that were previously classified for their salt sensitivity status. The present application discloses distinct patterns of selected exosomal miRNA expression that were different between salt-sensitive (SS), salt-resistant (SR), and inverse salt-sensitive (ISS) individuals. These miRNAs can be useful as biomarkers either individually or as panels comprising multiple miRNAs. The present invention provides compositions and methods for identifying, diagnosing, monitoring, and treating subjects with salt sensitivity of blood pressure. The applications discloses panels of miRNAs useful for comparing profiles, and in some cases one or more of the miRNAs in a panel can be used. The miRNAs useful for distinguishing SS and SR or ISS and SR subjects. One or more of the 45 miRNAs can be used. Some of the miRNAs have not been previously reported to be circulating. See those miRNAs with asterisks in FIG. 1 and below. The present invention encompasses the use of one or more of these markers for identifying and diagnosing SR, SS, and ISS subjects.
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(2015/02/05)

IMPROVED PROCESS FOR CRYSTALLIZATION OF BENAZEPRIL HYDROCHLORIDE
An improved process for the crystallization of benazepril hydrochloride to obtain in at least 99.8% diastereomeric purity. The process comprises making a concentrated solution of benazepril hydrochloride in ethanol and adding the resulting solution to a non-solvent diisopropyl ether.
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Page/Page column 4

(2009/04/23)

CRYSTALLINE POLYMORPHS OF BENAZEPRIL HYDROCHLORIDE
The present invention relates to a specific polymorph form of crystalline benazepril hydrochloride referred to as Form B, methods for producing this form of benazepril hydrochloride, compositions containing it, and methods for using it.
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Page/Page column 8; 21; 22

(2008/06/13)

BIS-DICARBOXYLIC ACID SALTS OF BENAZEPRIL AND PREPARATION OF BENAZEPRIL VIA THESE SALTS
Dicarboxylic acid salts of compounds of the formula (II) wherein R represents a selectively removable protecting group; and (S) denotes the (S)-configuration of the asymmetric carbon atoms, which are useful as intermediates for the preparation of benazepril or pharmaceutically acceptable salts thereof.
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Page/Page column 7

(2008/06/13)

PROCESS FOR PREPARATION OF BENAZEPRIL
The present invention relates to an improved process for preparation of highly pure benazepril of Formula I, wherein R is hydrogen or pharmacologically acceptable salt thereof by completely eliminating the impurity of 7-bromo analogue of benazepril of Formula Ia, wherein R is bromo group.
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Page/Page column 16-17

(2008/06/13)

Asymmetric synthesis of ACE inhibitor-Benazepril HCl via a bioreductive reaction
An enantioselective synthesis of the potent angiotensin converting enzyme (ACE) inhibitor (2S, 3′S)-2-(1-carboxymethyl-2-oxo-2,3,4,5-tetrahydro-1H- benzo[b]azepin-3-ylamino)-4-phenylbutyric acid ethyl ester hydrochloride, Benazepril HCl 4, has been achieved through an asymmetric reduction of 4-(2-nitrophenyl)-2,4-dioxobutyric acid ethyl ester 6b employing baker's yeast as the reductive catalyst.
Chang, Ching-Yao,Yang, Teng-Kuei
p. 2239 - 2245
(2007/10/03)

3-Amino-[1]-benzazepin-2-one-1-alkanoic acids
Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-ones and functional derivatives are angiotensin converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.
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(2008/06/13)

Synthesis and biological properties of (carboxyalkyl)amino-substituted bicyclic lactam inhibitors of angiotensin converting enzyme
Syntheses of the potent angiotensin converting enzyme inhibitor (3S)-1-(carboxymethyl)-3-[[(1S)-1-carboxy-3-phenylpropyl]amino]-2,3,4,5 -tetrahydro-1H-[1]benzazepin-2-one (CGS 14831) and the related monoester prodrug (17a; CGS 14824A) are described together with preparative details for six- and eight-membered ring analogues. Inhibitory potencies and in vivo biological activity of the compounds are discussed. The data indicate that 17a has a biological profile comparable to that of enalapril.
Watthey,Stanton,Desai,Babiarz,Finn
p. 1511 - 1516
(2007/10/02)

3-Amino-[1]-benzazepin-2-one-1-alkanoic acids
Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-ones and functional derivatives are angiotension converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.
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(2008/06/13)