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Novel gall bladder contraction poison receptor antagonist analogue and synthetic method thereof

The technology of a receptor antagonist and a synthesis method is applied in the synthesis of novel aspenisin analogs and the field of synthesis thereof, which can solve the problems of inconvenience in taking, short half-life and the like, and achieve a short route, simple separation and high yield. Effect

Inactive Publication Date: 2016-04-27
JIANGSU UNIV OF TECH
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

During the clinical use of many drugs, they are restricted or eliminated due to various defects, such as short half-life, which leads to inconvenience in taking, etc.

Method used

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  • Novel gall bladder contraction poison receptor antagonist analogue and synthetic method thereof
  • Novel gall bladder contraction poison receptor antagonist analogue and synthetic method thereof
  • Novel gall bladder contraction poison receptor antagonist analogue and synthetic method thereof

Examples

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Embodiment 1

[0026] A novel cholecystokinin receptor antagonist analog, which has the following structure:

[0027]

[0028] Example 1

[0029] A synthetic method of a novel cholecystokinin receptor antagonist analog, comprising the following steps:

[0030] 1) At room temperature, dissolve 5-methoxyisatoic acid rod (5.79g, 30mmol) in an aqueous solution of triethylamine (triethylamine 4.2mL, water 30mL) to make a 1.0mol / L solution, and then add L-Methionine (4.5g, 30mmol), the reactant was stirred at room temperature for 5 hours, concentrated under reduced pressure to remove water, and pumped to dryness. The intermediate was directly used as the raw material for the next step without separation and purification.

[0031] 2) Add the intermediate in the previous step into DMSO (1000mL) and heat and stir at 135-150°C for 5 hours, then cool to 0°C, add 1000mL of ice water under cooling, and extract with ether (150mL×6), combine organic phase, washed with saturated sodium chloride solutio...

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Abstract

The invention relates to a novel gall bladder contraction poison receptor antagonist analogue with a structure as shown in the specification. A synthetic method of the novel gall bladder contraction poison receptor antagonist analogue includes enabling L-methionine, serving as a raw material, to react with 5-methylisatoic anhydride to obtain seven-membered ring lactam, performing selective acylation on the seven-membered ring lactam and substitutional benzoyl chloride, and performing nitro-reduction and dehydration to form quinazolinone rings to further obtain the novel gall bladder contraction poison receptor antagonist analogue. The obtained target compound is brand new, synthetic route is short, operation and separation in each step are simple, yield is high, reagents are common and cheap, and accordingly, the compound is suitable for mass production.

Description

technical field [0001] The present invention relates to the synthesis of a novel aspenisin analog and its synthesis method, in particular to a novel cholecystokinin receptor antagonist analog and its synthesis method. Background technique [0002] On the basis of existing drugs, it is of great scientific and practical significance for the development of new drugs to use organic synthesis to design synthetic drugs and their derivatives, and to carry out drug screening in combination with biological activity tests. During the clinical use of many drugs, they are restricted or eliminated due to various defects, such as short half-lives, which lead to inconvenience in taking them. Therefore, in order to increase drug efficacy, improve absorption, prolong action time and reduce side effects, it is one of the main sources of new drug research and development to study some drugs that have been used in clinical practice as lead compounds. The well-known cystokinin antagonist devaze...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04
CPCC07D487/04
Inventor 杨廷海罗世鹏刘维桥周全法
Owner JIANGSU UNIV OF TECH
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