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Method for synthesizing isradipine medicament midbody 4-formyl benzo furazan

A technology of formylbenzene and isradipine, which is applied in the field of synthesizing isradipine pharmaceutical intermediate 4-formylbenzofurazan, can solve the problems of high price and high production cost, and achieve low cost, short production cycle, and high yield. high rate effect

Inactive Publication Date: 2013-09-25
江苏倍达医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] This method will use expensive 4-(dibromomethyl)benzofurazan and silver nitrate, and the production cost is higher

Method used

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  • Method for synthesizing isradipine medicament midbody 4-formyl benzo furazan
  • Method for synthesizing isradipine medicament midbody 4-formyl benzo furazan
  • Method for synthesizing isradipine medicament midbody 4-formyl benzo furazan

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specific Embodiment 1

[0018] Specific embodiment one: a method for synthesizing isradipine pharmaceutical intermediate 4-formylbenzofurazan 1, the method is: 10.3g 4-methylbenzofurazan 2 is dissolved in 50ml acetic acid, and 1ml is added Water and 9.3g of selenium dioxide, stirred and heated to 100°C, reacted for 6 hours, cooled to room temperature, filtered the reaction solution, washed the filter residue 3 times with ethyl acetate, concentrated the mother liquor to about 15ml, then poured it into 200ml of water, The product was extracted with ethyl acetate, the organic phase was washed three times with saturated brine, the organic phase was dried, and concentrated to dryness, the obtained crude product was recrystallized from a mixed solution of ethyl acetate and petroleum ether to obtain 9.5 g of light yellow solid product-formylbenzene And Furazan 1.

[0019]

specific Embodiment 2

[0020] Specific example two: a method for synthesizing isradipine drug intermediate 4-formylbenzofurazan 1, the method is: 10.3g 4-methylbenzofurazan 2 is dissolved in 50ml 1,4-diox Add 1ml of water and 9.3g of selenium dioxide to the six rings, stir and heat to 100°C, react for 6 hours, cool to room temperature, filter the reaction solution, wash the filter residue 3 times with ethyl acetate, concentrate the mother liquor to about 15ml, Then pour it into 200ml of water, extract the product with ethyl acetate, wash the organic phase three times with saturated brine, dry the organic phase, and concentrate to dryness. The resulting crude product is recrystallized from a mixed solution of ethyl acetate and petroleum ether to obtain 9.5 g of light yellow Solid product - formylbenzofurazan 1.

[0021]

specific Embodiment 3

[0022] Specific example three: a method for synthesizing isradipine drug intermediate 4-formylbenzofurazan 1, the method is: 10.3g 4-methylbenzofurazan 2 is dissolved in 25ml acetic acid and 25ml1,4 -In the mixed solution of dioxane, add 1ml of water and 9.3g of selenium dioxide, stir and heat to 100°C, react for 6 hours, cool to room temperature, filter the reaction solution, wash the filter residue 3 times with ethyl acetate, and Concentrate the mother liquor to about 15ml, then pour it into 200ml of water, extract the product with ethyl acetate, wash the organic phase three times with saturated brine, dry the organic phase, concentrate to dryness, and recrystallize the obtained crude product with a mixed solution of ethyl acetate and petroleum ether , to obtain 9.5 g of light yellow solid product-formylbenzofurazan 1.

[0023]

[0024] The invention relates to a method for synthesizing isradipine drug intermediate 4-formylbenzofurazan. The method has the characteristics ...

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Abstract

The invention relates to a method for synthesizing an isradipine medicament midbody 4-formyl benzo furazan. The method comprises a step of preparing the 4-formyl benzo furazan by using reagents of 4-methyl benzo furazan, an oxidant selenium dioxide and the like. The method has the characteristics of low cost, high yield, short production period and the like. In addition, the reaction condition of the method is easy to realize and control, and the industrial production is facilitated.

Description

technical field [0001] The invention relates to a method for synthesizing isradipine drug intermediate 4-formylbenzofurazan. Background technique [0002] 4-Formylbenzofurazan, also known as benzofurazan-4-carbaldehyde or 4-formylbenzofurazan, chemical name: 2,1,3-benzoxadiazole-4-carbaldehyde, English Name: Benzofrazan-4-carbaldehyde, which is an important intermediate in the synthesis of antihypertensive drug isradipine. Isradipine, English name: Isradine, is a dihydropyridine calcium antagonist with high selectivity to blood vessels, can relax peripheral blood vessels, coronary blood vessels and cerebrovascular, has little effect on the heart, and only inhibits the sinoatrial node of spontaneous activities. It is a new class of antihypertensive drugs. In recent years, domestic and foreign studies on the synthesis of isradipine and its intermediates have been going on, and the present invention mainly improves the synthesis of its important intermediate 4-formylbenzofur...

Claims

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Application Information

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IPC IPC(8): C07D271/12
Inventor 张晓霞肖刚刚娄山宁陈维忠符亚亮
Owner 江苏倍达医药科技有限公司
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