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Olmesartan medoxomil compound and preparation method thereof

A technology for olmesartan medoxomil and hydrate, which is applied in the field of chemical preparation, can solve the problems of insufficient product stability, high production cost, long production cycle and the like, and achieves the effects of increasing stability, reducing production cost and extending validity period.

Active Publication Date: 2014-12-10
GUIPING PRODIVITY PROMOTION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, olmesartan medoxomil is synthesized by chemical methods, and there are deficiencies such as low molar yield, long production cycle, high production cost, unstable product, and short validity period in the synthetic method.

Method used

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  • Olmesartan medoxomil compound and preparation method thereof
  • Olmesartan medoxomil compound and preparation method thereof
  • Olmesartan medoxomil compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Get 20kg4-(1-hydroxyl-1-methylethyl)-2-propylimidazole-5-carboxylic acid ethyl ester, 10kg calcium oxide, 40kg4-[2-(trityl tetrazol-5-yl) Phenyl] benzyl bromide, 2kg of triazole, 100kg of N,N-dimethylacetamide, placed in a sonochemical reactor, select ultrasonic frequency 20kHz, react at room temperature for 1 hour, filter, pour the filtrate into 500kg of ice-water mixture medium, crystallize, filter, pour the filter residue into 500kg of acetone, select ultrasonic frequency 10kHz, dissolve, filter, cool the filtrate to 0°C, filter, dry the filter residue at 60°C, add 4kg of sodium hydroxide, 300kg of N,N-dimethyl Acetamide, select ultrasonic frequency 20kHz, react at room temperature for 30 minutes, cool the reaction mixture to 0°C, add 7kg of potassium carbonate, 1kg of tetramethylethylenediamine, 20kg of 4-chloromethyl-5-methyl-2-oxo- 1,3-dioxol-2-one, 30kg N,N-dimethylacetamide, heat the reactant to 80°C, keep the reaction for 2 hours, cool the reaction mixture to 5...

specific Embodiment 2

[0036] Get 20kg4-(1-hydroxyl-1-methylethyl)-2-propylimidazole-5-carboxylic acid ethyl ester, 10kg calcium oxide, 40kg4-[2-(trityl tetrazol-5-yl) Phenyl] benzyl bromide, 2kg of triazole, 100kg of N,N-dimethylacetamide, placed in a sonochemical reactor, select ultrasonic frequency 30kHz, react at room temperature for 1 hour, filter, pour the filtrate into 500kg of ice-water mixture medium, crystallize, filter, pour the filter residue into 500kg of acetone, select ultrasonic frequency 20kHz, dissolve, filter, cool the filtrate to 4°C, filter, dry the filter residue at 60°C, add 4kg of sodium hydroxide, 300kg of N,N-dimethyl Acetamide, select ultrasonic frequency 30kHz, react at room temperature for 30 minutes, cool the reaction mixture to 0°C, add 7kg of potassium carbonate, 1kg of tetramethylethylenediamine, 20kg of 4-chloromethyl-5-methyl-2-oxo- 1,3-dioxol-2-one, 30kg N,N-dimethylacetamide, heat the reactant to 80°C, keep the reaction for 2 hours, cool the reaction mixture to 5...

specific Embodiment 3

[0038]Get 20kg4-(1-hydroxyl-1-methylethyl)-2-propylimidazole-5-carboxylic acid ethyl ester, 10kg calcium oxide, 40kg4-[2-(trityl tetrazol-5-yl) Phenyl] benzyl bromide, 2kg of triazole, 100kg of N,N-dimethylacetamide, placed in a sonochemical reactor, select ultrasonic frequency 25kHz, react at room temperature for 1 hour, filter, pour the filtrate into 500kg of ice-water mixture medium, crystallize, filter, pour the filter residue into 500kg of acetone, select ultrasonic frequency 15kHz, dissolve, filter, cool the filtrate to 2°C, filter, dry the filter residue at 60°C, add 4kg of sodium hydroxide, 300kg of N,N-dimethyl Acetamide, select ultrasonic frequency 25kHz, react at room temperature for 30 minutes, cool the reaction mixture to 0°C, add 7kg of potassium carbonate, 1kg of tetramethylethylenediamine, 20kg of 4-chloromethyl-5-methyl-2-oxo- 1,3-dioxol-2-one, 30kg N,N-dimethylacetamide, heat the reactant to 80°C, keep the reaction for 2 hours, cool the reaction mixture to 5°...

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Abstract

The invention discloses an olmesartan medoxomil compound and a preparation method thereof, and particularly relates to a new olmesartan medoxomil compound which is prepared through synthesis and crystallization under ultrasonic condition in the presence of triazole and tetramethylethylenediamine as catalysts, and a preparation method thereof, wherein the preparation method has the characteristics of moderate reaction conditions, high yield of product, short reaction time, good stability of product and prolonged period of validity; and as a result, satisfying effects are achieved.

Description

technical field [0001] The invention relates to the field of chemical medicine preparation, in particular to an olmesartan medoxomil compound and a preparation method thereof. Background technique [0002] Olmesartan medoxomil is an ideal antihypertensive drug, which has good curative effect on various types of hypertension, and has obvious advantages such as small dose, quick onset, strong antihypertensive effect, and low incidence of adverse reactions. At present, olmesartan medoxomil is synthesized by a chemical method, and there are disadvantages such as low molar yield, long production cycle, high production cost, unstable product and short validity period in the synthetic method. Contents of the invention [0003] In order to overcome the above-mentioned deficiencies, the present invention explores and optimizes the synthesis process of olmesartan medoxomil, adopts triazole and tetramethylethylenediamine as catalysts, synthesizes under ultrasonic conditions, crystall...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D405/14
Inventor 孙威
Owner GUIPING PRODIVITY PROMOTION CENT