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Preparation method of general intermediate ECPPA of ACEI (angiotensin converting enzyme inhibitor) medicines

A technology of intermediates and puli, applied in the field of preparation of pharmaceutical intermediates, can solve the problem of high cost of precious metal catalysts, and achieve the effects of improving yield, reducing costs and reducing separation steps

Inactive Publication Date: 2013-11-20
大连鼎燕医药化工有限公司 +1
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Problems solved by technology

However, the cost of precious metal catalysts applied in the final hydrogenation step is high

Method used

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  • Preparation method of general intermediate ECPPA of ACEI (angiotensin converting enzyme inhibitor) medicines
  • Preparation method of general intermediate ECPPA of ACEI (angiotensin converting enzyme inhibitor) medicines
  • Preparation method of general intermediate ECPPA of ACEI (angiotensin converting enzyme inhibitor) medicines

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preparation example Construction

[0030] The preparation method of the universal intermediate ECPPA of the pril class medicine of the present invention, the steps are as follows:

[0031]

[0032] (1) Synthesis of benzoyl acrylic acid

[0033] Mix benzene and maleic anhydride, the dosage ratio of benzene and maleic anhydride is 800g: 135-143g, stir to dissolve;

[0034] Slowly add aluminum trichloride, the dosage ratio of benzene to aluminum trichloride is 800g: 555-605g, heat up and reflux for 55-65 minutes, and cool down to room temperature;

[0035] Slowly pour the reaction solution into a mixture of concentrated hydrochloric acid and crushed ice. The ratio of concentrated hydrochloric acid to crushed ice is 1-3 liters: 3kg, and the ratio of benzene to the mixture is 800g: 555-605ml; filter and dry to obtain a brown solid Granules, yield 98%, mp: 90~93℃, HPLC≥95%;

[0036] (2) Synthesis of ethyl benzoyl acrylate

[0037] Mix the benzoyl acrylic acid, ethanol, and boron trifluoride etherate complex syn...

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Abstract

The invention relates to a preparation method of a general intermediate ECPPA of ACEI medicines. The method comprises the steps of preparing benzoylacrylic acid, preparing ethyl benzoylacrylate, preparing L-alanine benzyl ester p-toluenesulfonate, preparing N-((S)-1-ethoxycarbonyl-3-acetylphenyl)-L-alanine benzyl ester, and preparing N-((S)-1-ethoxycarbonyl-3-phenylpropyl)-L-alanine. Compared with the prior art, the method provided by the invention has the advantages of product yield increase, raw material cost reduction, separation step reduction, and catalyst cost reduction.

Description

technical field [0001] The invention relates to a preparation method of a drug intermediate, in particular to a preparation method of ECPPA, a universal intermediate of pulil drugs. Background technique [0002] ECPPA is a common intermediate of pril-type hypertension drugs, and more than a dozen pril-type drugs can be synthesized from it. Like dipine and sartan drugs, pril drugs are one of the three series of drugs for hypertension. [0003] Because of its importance, the world's medical community has paid great attention to this active intermediate compound, and has successively researched and developed the following process routes: [0004] Route 1: Journal of Labeled Compounds and Radiopharmaceuticals, 23(7), 771-6; 1986. [0005] The process uses bromoethylbenzene as the raw material, produces Grignard reagent through Grignard reaction, and then condenses with oxalic acid ester, and undergoes oximation with the amino group on alanine and hydrogenation reduction of s...

Claims

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Application Information

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IPC IPC(8): C07C229/34C07C227/18
Inventor 张洪学刘英张勇汪洋姜人武张绥英吴冬辉李德龙
Owner 大连鼎燕医药化工有限公司
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