Preparation method for efonidipine

An efodipine and recrystallization technology, which is applied in chemical instruments and methods, compounds of group 5/15 elements of the periodic table, organic chemistry, etc., can solve the problems of complex production process and low yield, and achieve good product quality, The effect of simple manufacturing process

Inactive Publication Date: 2015-07-01
蒋学京
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the current production of efodipine, the production process is complicated and the output is low

Method used

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Embodiment Construction

[0006] Now in conjunction with the present invention for further detailed description.

[0007] A kind of preparation method of efodipine of the present invention, concrete steps are as follows: 2,2-dimethylpropene α-(3-nitrobenzyl) acetonyl phosphate and 2-(N-benzyl-N- Phenylamino) ethyl 3-aminobutenoic acid ester was dissolved in toluene, refluxed for 10 h, the precipitate was collected by filtration, and recrystallized with ethyl acetate to obtain efodipine.

[0008] Uses of Efodipine: dihydropyridine calcium ion antagonist, with L-type and T-type calcium channel blocking effects; used for the treatment of essential hypertension, severe hypertension and renal hypertension.

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Abstract

The invention relates to a preparation method for efonidipine. The preparation method comprises the following concrete steps: dissolving 2,2-dimethylpropylene-alpha-(3-nitrobenzenyl)acetonyl phosphate and 2-(N-benzyl-N-phenylamino)ethyl-3-amino butenoic acid ester in toluene; carrying out a reflux reaction for 10 h; carrying out filtering and collecting a precipitate; and subjecting the precipitate to recrystallization with ethyl acetate so as to obtain efonidipine. The preparation method for efonidipine is simple, and prepared efonidipine has good quality.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a preparation method of efodipine. Background technique [0002] Efodipine is a calcium antagonist that introduces phosphorus chloride into dihydropyridines. It has the effect of selectively increasing the sensitivity of dihydropyridine receptors, thereby continuously lowering blood pressure. Chest opening of dogs under anesthesia, it can be seen that this product increases blood flow of coronary artery and vertebral artery. And observed that this product can reduce the total peripheral vascular resistance, increase cardiac output and stroke volume. Observation of dogs without anesthesia shows that this product can reduce renal vascular resistance and increase renal blood flow. Under anesthesia, it can be observed that this product can lower the blood pressure of spontaneously hypertensive rats, even if the spinal cord is damaged, the blood pressure can also be seen to drop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6574
Inventor 蒋学京
Owner 蒋学京
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