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Preparation method of naftidrofuryl oxalate

A technology of naphthofuramide oxalate and tetrahydrofuran propionic acid, which is applied in the field of pharmaceutical synthesis, can solve the problems of high price of compound a, low product purity, complicated processing process, etc., and achieves high pressure, high purity and high equipment requirements. Effect

Inactive Publication Date: 2014-10-08
刘博
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] 2. In (Pharmaceutical.substances.4th.ed.) edited by kleemann & Engel, it uses the compound of structural formula b and the compound of structural formula d as starting materials, through alkylation, and then with the compound alkyl of structural formula e Alkylation, hydrolysis and decarboxylation first, and then esterification with a compound of structural formula f to synthesize the target product; the price of compound a is high, and the post-alkylation treatment process is cumbersome, the amount of waste water is large, and the product purity is not high

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  • Preparation method of naftidrofuryl oxalate
  • Preparation method of naftidrofuryl oxalate
  • Preparation method of naftidrofuryl oxalate

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Embodiment Construction

[0039] The present invention will be further described in detail below through the specific examples, the following examples are only descriptive, not restrictive, and cannot limit the protection scope of the present invention with this.

[0040] The reaction scheme that the present invention relates to is as follows:

[0041]

[0042] A kind of preparation method of naphthurinate oxalate, the steps are as follows:

[0043]1. Add 320g of diethyl malonate, 211g of furfural and 1000mL of toluene to the reaction flask, add dropwise 10mL of piperidine and 20mL of glacial acetic acid, after the addition is completed, heat up and reflux for water separation reaction. The reaction time is 3 hours. After the reaction is completed, cool to At room temperature, wash 3 times with 300mL deionized water, take the upper organic layer, dry over anhydrous sodium sulfate, reclaim toluene by distillation under reduced pressure, until no toluene goes out, and obtain yellow oily furyl methylen...

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Abstract

The invention relates to a preparation method of naftidrofuryl oxalate. During preparation of a compound, namely, furanmethylenediethyl malonate (II), cheap and readily-available furfural and malonic acid diethyl acetate are selected as starting raw materials. By means of process optimization, the synthesis conditions of the compound II are mild, the operation is easy and the purity and yield are high. The defects of trouble in treatment after an alkylation reaction, high impurity content and low purity due to the adoption of high-price 2-chloromethyl tetrahydrofuran as a raw material in the conventional process are overcome.

Description

technical field [0001] The invention belongs to the field of pharmaceutical synthesis methods, and relates to a preparation method of a vasodilator and an antispasmodic agent, in particular to a preparation method of nafuramide oxalate. Background technique [0002] Naftidrofuryl oxalate, chemical name alpha-(1-naphthylmethyl)-2-tetrahydrofuran propionate diethylaminoethyl oxalate, English name alpha-(1-Naphthylmethyl)- 2-tetrahydrofuran propionic acid diethylaminoethyl ester oxalate, the structural formula (I) is shown below. [0003] [0004] Nafifuramide oxalate is a dilator of cerebrovascular and peripheral blood vessels; antagonizes the effects of serotonin and bradykinin; can increase intracellular ATP to improve cell metabolism; reduce blood and plasma viscosity and fibrin Original concentration; increase the oxidative capacity of cells and protect cells from hypoxia; in addition, it has a papaverine-like antispasmodic effect, which is slow and long-lasting. [0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/16
CPCC07D307/16
Inventor 刘博
Owner 刘博