Method for preparing N-[2-(1-ethoxycarbonyl-3-phenylpropylamino)-tauryl]-thiazolidinecarboxylic acid and its derivant

A derivative, thiazolidine technology, applied in the field of preparation of N-[2-(1-ethoxyacyl-3-phenylpropylamino)-tauryl]-thiazolidine acid and its derivatives, can solve the problem of blood pressure elevation advanced questions

Inactive Publication Date: 2008-09-24
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Problems solved by technology

Angiotensin source is a glycoprotein. After the action of renin, angiotensin source composed of 453 amino acids is cleaved to release 10 amino acid inactive polypeptide angiotensin I (AngI). Convert enzyme enzymatic hydrolysis to obtain octapeptide angiotensin II (AngII), and angiotensin II can stimulate the adrenal gland to release aldosterone and constrict blood vessels, resulting in increased blood pressure

Method used

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  • Method for preparing N-[2-(1-ethoxycarbonyl-3-phenylpropylamino)-tauryl]-thiazolidinecarboxylic acid and its derivant
  • Method for preparing N-[2-(1-ethoxycarbonyl-3-phenylpropylamino)-tauryl]-thiazolidinecarboxylic acid and its derivant
  • Method for preparing N-[2-(1-ethoxycarbonyl-3-phenylpropylamino)-tauryl]-thiazolidinecarboxylic acid and its derivant

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Embodiment Construction

[0018] The experimental steps are as follows:

[0019] Synthesis of Thiazolidine Acid and Its Derivatives [15]

[0020] L-cysteine ​​hydrochloride, K AC , ethanol and water are mixed in a certain proportion, aldehyde compounds are added, stirred, crystallized, suction filtered, washed and dried to obtain a crude product, purified and dried to obtain a white crystal.

[0021] Synthesis of Benzyl Thiazolidine Acid [16]

[0022] Suspend thiazolidinic acid and its derivatives in benzyl alcohol, add thionyl chloride dropwise under stirring in an ice bath, distill thionyl chloride under reduced pressure after the reaction is completed, filter, wash the filtrate with water, adjust the pH value with saturated potassium carbonate, dichloride Extracted with methane, dried the organic layer, and rotary evaporated to obtain the compound.

[0023] dipeptide production

[0024] Dissolve BOC-taurine in THF, add HoBt, thiazolidinic acid and its derivative hydrochloride and N-ethylmorpho...

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Abstract

According to the conception of a novel drug design, the present invention provides improved decoration based on the existing ACEI and relates to a design comprising the following two types of conception: first, the toxic side-effect points of the existing ACEI are avoided to the greatest extent; secondly, the effects of the ACEI are improved to the greatest extent. Thus the present invention provides a novel ACEI compound. Based on the basic structure of enalapril, the present invention provides a synthetic route for improving decoration. The structure of propanamine-sulfonyl is changed into cattle sulphonyl; the praline is changed into timonacic acid and derivatives thereof, so as to prepare a series of compounds, namely, N-[2-(1-ethoxycarbonyl-3-phenylalanine)-cattle-sulfonyl]-timonacic acid and derivatives thereof. The drugs are screened to prepare novel high-efficiency and low-toxicity ACEI.

Description

technical field [0001] organic chemistry Background technique [0002] Angiotensin Converting Enzyme Inhibitor (ACEI) mainly acts on the renin-angiotensin system (Renin-Angiotensin System, RAS) and inhibits the activity of angiotensin converting enzyme. The renin-angiotensin system plays an important role in the regulation of blood pressure. Angiotensin-converting enzyme is a membrane-immobilized metalloprotease, which contains 1306 amino acids, and the results show that the active center contains a Zn 2+ , protonated arginine and a hydrophobic cavity. Physiologically, it is a key enzyme in the renin-angiotensin system that regulates blood pressure in the body. Angiotensin source is a glycoprotein. After the action of renin, angiotensin source composed of 453 amino acids is cleaved to release 10 amino acid inactive polypeptide angiotensin I (AngI). Convert enzyme enzymatic hydrolysis to obtain octapeptide angiotensin II (AngII), and angiotensin II can stimulate the adren...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/06A61K31/426A61P9/12
CPCY02P20/584
Inventor 代斌张洁刘志勇顾承志仲伶俐王东马晓伟
Owner 代斌
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