Amorphous lercanidipine hydrochloride and preparation method thereof

An amorphous technology of lercanidipine hydrochloride, which is applied in the field of high-purity amorphous lercanidipine hydrochloride and its preparation, can solve the problems of unsuitability for industrial production, cumbersome operation, and long cycle, and achieve easy commercial industrial scale implementation , high purity, short cycle effect

Active Publication Date: 2014-02-26
CHINA RESOURCES SAIKE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above method has high cost, long period and cumbersome operation in the process of commercialization, and is not suitable for industrial production.

Method used

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  • Amorphous lercanidipine hydrochloride and preparation method thereof
  • Amorphous lercanidipine hydrochloride and preparation method thereof
  • Amorphous lercanidipine hydrochloride and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1: Preparation of free state lercanidipine base solution

[0050] Add 20g of crude lercanidipine hydrochloride into 100mL of dichloromethane, adjust the pH to 7.5-8.0 with saturated aqueous sodium bicarbonate solution at 5°C under stirring, leave to stand for layers, and separate the organic layer to obtain free lercanidipine The base dichloromethane solution is set aside.

Embodiment 2

[0051] Embodiment 2: the preparation of lercanidipine oxalate crude product

[0052] Add 30ml of an aqueous solution of 2.9g oxalic acid to the lercanidipine base dichloromethane solution prepared in Example 1, stir well and separate the organic phase, dry it over anhydrous sodium sulfate, vacuum filter and evaporate to dryness to obtain Lercani Crude dipine oxalate (yield = 18.6 g, HPLC purity: 98.6%).

Embodiment 3

[0053] Embodiment 3: primary crystallization of lercanidipine oxalate

[0054] Dissolve 10g of crude lercanidipine oxalate in 50ml of ethanol at 80°C under stirring in a dry reaction bottle, slowly cool to 20°C, stir at a medium speed for 8 hours, a pale yellow solid precipitates, filter, and wash twice with 10ml of ethanol , air-dried at 45° C. to obtain a light yellow solid (yield = 7.6 g, HPLC purity: 99.6%).

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Abstract

Lercanidipine hydrochloride is the third generation of dihydrophridine calcium antagonist and mainly used for treating hypertension and angina clinically. The amorphous lercanidipine hydrochloride is easy to smash, and the purity of the amorphous lercanidipine hydrochloride is at least 98.5%, higher purity is at least 99.5%, and the highest purity is at least 99.7%. The invention further provides a preparation method for the high purity amorphous lercanidipine hydrochloride.

Description

Technical field: [0001] The invention relates to a high-purity amorphous lercanidipine hydrochloride and a preparation method thereof. Clinically used for antihypertensive. Background technique: [0002] Lercanidipine Hydrochloride, a third-generation dihydropyridine calcium antagonist developed for the Italian Recordati company, was first listed in the Netherlands in December 1997, with the trade name Zanidip, and was launched in the UK, Italy, and Greece in 1998. It was subsequently launched in other European countries. [0003] Lercanidipine hydrochloride is a third-generation dihydropyridine calcium antagonist, which can reversibly block the Ca2+ inflow of L-type calcium channels in vascular smooth muscle cell membranes, dilate peripheral blood vessels and lower blood pressure. Highly lipophilic dihydropyridine calcium antagonist. Its antihypertensive mechanism is to block the calcium channel of arterial vascular smooth muscle and directly relax the vascular smooth mu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/90A61K31/4422A61P9/12
Inventor 刘意林祁伟杨琰
Owner CHINA RESOURCES SAIKE PHARMA
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