Process for preparing milrinone

A technology of acetone and triethyl orthoformate, applied in the direction of organic chemistry, can solve the problems of expensive raw materials, complex synthesis lines, and high equipment requirements, and achieve the effects of simplifying operations, simplifying the process, and reducing production costs

Inactive Publication Date: 2006-04-26
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there are generally disadvantages such as complex synthesis lines, high equipment requirements, expensive raw materials and not easy to obtain.

Method used

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  • Process for preparing milrinone
  • Process for preparing milrinone

Examples

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example 1

[0017] Put 147g of 1-(4-pyridyl)-acetone, 235ml of glacial acetic acid, 195ml of acetic anhydride, and 300ml of triethyl orthoformate into a 3-liter three-necked flask, install a thermometer, stir, and continue to react at room temperature for 15 hours, then reduce the pressure After concentrating, add 1500ml of ethanol and 120g of α-cyanoacetamide in sequence, adjust the pH to ≥10 with 2N NaOH aqueous solution at 0°C, filter, soak the filter cake once with ethanol, drain, and dry to obtain 181.2g of crude product, which is used later DMF was recrystallized, and 151.8 g of fine milrinone was collected with a yield of 66%.

example 2

[0019] Put 100g of 1-(4-pyridyl)-acetone, 180ml of glacial acetic acid, 160ml of acetic anhydride, and 195ml of triethyl orthoformate into a 3-liter three-necked flask, install a thermometer, stir, and continue to react at room temperature for 15 hours. After concentrating, add 1000ml of tetrahydrofuran and 90g of α-cyanoacetamide in sequence, adjust the pH to ≥ 11 with 2N NaOH aqueous solution at 0°C, filter, soak the filter cake once with ethanol, drain, and dry to obtain 121g of crude product, which is then washed with DMF After recrystallization, 99.4 g of fine milrinone was collected with a yield of 63.5%.

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Abstract

The present invention uses 1-(4-pyridyl)-acetone as a raw material for condensation reaction with triethyl orthoformate, and the condensate is directly cyclized with α-cyanoacetamide to obtain milrinone without purification, and is characterized in that The "one-pot" process is adopted, and the intermediate product is not purified. Milrinone is an important chemical product, which can be used as a cardiotonic drug, etc.

Description

technical field [0001] The invention relates to a preparation method of the compound milrinone (1,6-dihydro-2-methyl-6-oxo-[3,4`-bipyridine]-5-carbonitrile), which belongs to the field of chemical industry and chemical medicine . Background technique [0002] Milrinone (Milirinone, 1) is the general name of -1,6-dihydro-2-methyl-6-oxo-[3,4`-bipyridine]-5-carbonitrile, and its structural formula is: [0003] [0004] Milrinone is a second-generation bispyridine cardiotonic drug launched in the United States in 1987. Milrinone is a homologue of amrinone. It has higher selectivity to phosphodiesterase III, and its cardiotonic activity is 10 to 30 times that of amrinone. It has few adverse reactions and is effective when taken orally. Therefore, since the drug was launched, many companies have completed the preparation of milrinone through multiple routes. However, there are generally disadvantages such as complex synthesis lines, high equipment requirements, expensive raw...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/84
Inventor 赵志全
Owner LUNAN PHARMA GROUP CORPORATION
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