Nisoldipine compound and novel preparation method thereof

A technology for nisoldipine and a compound, which is applied in the field of nisoldipine compounds and new preparation methods thereof, can solve the problems of unsatisfactory drug purity, no public purification method, and reduced content of drug active ingredients, and achieves the improvement of clinical adverse reactions. Effect
CN102491940BInactive Publication Date: 2013-03-06HAINAN MEILAN SMITH KLINE PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HAINAN MEILAN SMITH KLINE PHARMA
Publication Date
2013-03-06
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a high purity nisoldipine compound, which comprises the following steps: (1) dissolving a certain amount of rough nisoldipine products in an organic solvent, adding activated carbon into the organic solvent to absorb and filter, collecting filtrate, and reducing pressure and concentrating to obtain primary purified nisoldipine; (2) separating and purifying the primary purified nisoldipine by using a preparation type chromatographic column, and collecting eluent to obtain secondary purified nisoldipine; and (3) decompressing and concentrating the eluent, adding water while stirring, performing heating and backflow, performing cooling and crystallization, and centrifugally washing and drying precipitated crystals to obtain tertiary purified nisoldipine. By means of the method, the nisoldipine produced has high purity, the toxic and side effects of prepared pharmaceuticals for treating hemorrhagic cerebrovascular diseases, high blood pressure and the like are reduced, product quality of preparation is improved, and the high purity nisoldipine compound is suitable for large-scale industrialization production.
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Description

technical field

[0001] The invention relates to a nisoldipine compound and a new preparation method thereof, which can obtain a high-purity nisoldipine compound and belongs to the technical field of medicine. Background technique

[0002] Nisoldipine, yellow crystalline powder, chemical name: (±)-2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydro-3,5- Methyl picolinate isobutyl, molecular formula: C 20 h 24 N 2 o 6 , molecular weight: 388.41, the structural formula is as follows:

[0003]

[0004] Nisoldipine is currently the long-acting dihydropyridine calcium antagonist with the strongest selective vasodilation effect. Since the advent of nifedipine in 1971, more than 20 new drugs have been successfully developed. These drugs have the same mechanism of action (inhibition of Ca entry into tissue cells). Due to the difference in the binding properties of each compound to the receptor, the tissue selectivity is also different, and the pharmacological activity exhibited is a...

Claims

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