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Production method of malonic acid mono-p-nitrobenzyl ester as penem medicament intermediate

A technology of p-nitrobenzyl ester and p-nitrobenzyl malonate, which is applied in the field of penem drug intermediate p-nitrobenzyl malonate, which can solve the problems of high raw material cost, high price of nitrobenzyl alcohol and no market Competitiveness and other issues, to achieve the effect of high product yield, simple process and easy operation

Inactive Publication Date: 2011-12-14
江苏德峰药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The existing production of mono-p-nitrobenzyl malonate is obtained through esterification reaction of malonic acid and p-nitrobenzyl alcohol. This reaction is easy to generate dibenzyl malonate, and the price of p-nitrobenzyl alcohol High, so the cost of raw materials is high and there is no market competitiveness

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] In a 1000 ml three-necked flask equipped with a stirrer, a thermometer and a reflux condenser, add 296 grams of disodium malonate, 172 grams of p-nitrobenzyl chloride, 400 milliliters of acetonitrile, 101 grams of triethylamine, and stir under reflux 10 hours, then add 300 milliliters of water and stir, filter, the filtrate is layered, the oil layer is washed with aqueous sodium carbonate solution, and then washed with saturated brine to PH7, after distillation and concentration, a solid product is obtained, which is refined and dried with water to obtain 140 grams of the product, with a content of 98.5 %.

Embodiment 2

[0016] In a 1000 ml three-neck flask equipped with a stirrer, a thermometer and a reflux condenser, add 296 grams of disodium malonate, 172 grams of p-nitrobenzyl chloride, 400 milliliters of toluene, 101 grams of triethylamine, and stir to reflux 10 hours, then add 300 milliliters of water and stir, filter, the filtrate is layered, the oil layer is washed with aqueous sodium carbonate solution, and then washed with saturated brine to PH7, after distillation and concentration, a solid product is obtained, which is refined and dried with water to obtain 180 grams of the product, with a content of 98.5 %.

Embodiment 3

[0018] In a 1000 ml three-necked flask equipped with a stirrer, a thermometer and a reflux condenser, 296 grams of disodium malonate, 172 grams of p-nitrobenzyl chloride, 400 milliliters of toluene, 101 grams of triethylamine, 10 grams of Stir and reflux p-toluenesulfonic acid for 10 hours, then add 300 ml of water to stir, filter, and separate layers of the filtrate. The oil layer is washed with aqueous sodium carbonate solution, and then washed with saturated brine to pH 7. After distillation and concentration, a solid product is obtained, which is refined and dried with water to obtain Product 195 grams, content 98.5%.

[0019]

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PUM

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Abstract

The invention discloses a production method of malonic acid mono-p-nitrobenzyl ester as a penem medicament intermediate. The malonic acid mono-p-nitrobenzyl ester is generated through reaction in the existence of halogenated p-nitrobenzene and malonic acid or sodium salt thereof, a solvent, a catalyst and the like. The production method disclosed by the invention has the advantages of simple process, easiness for operation and high product yield.

Description

technical field [0001] The invention relates to a production method of penem medicine intermediate mono-p-nitrobenzyl malonate. Background technique [0002] The existing production of mono-p-nitrobenzyl malonate is obtained by esterification of malonic acid and p-nitrobenzyl alcohol. This reaction is easy to generate dibenzyl malonate, and the price of p-nitrobenzyl alcohol High, so the cost of raw materials is relatively high, and there is no market competitiveness. Contents of the invention [0003] The object of the present invention is to provide a kind of cheap raw material p-nitrobenzyl chloride as the basic raw material, and obtain monobenzyl malonate through reaction with excess malonic acid. [0004] Technical solution of the present invention is: [0005] A method for producing penem drug intermediate mono-p-nitrobenzyl malonate, characterized in that the reaction and Aftertreatment generates mono-p-nitrobenzyl malonate, reaction formula: [0006] . [00...

Claims

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Application Information

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IPC IPC(8): C07C205/43C07C201/12
Inventor 王德峰王炳才石飞朱小飞俞健钧
Owner 江苏德峰药业有限公司
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