Aspartic acid amlodipine compound and synthesis method thereof
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A technology of amlodipine aspartate and a synthesis method, which is applied in the field of amlodipine aspartate compound and its synthesis, can solve the problems of high production risk, low total yield, complicated process and the like, and achieves less toxic and side effects , the route is short, the effect of improving the compliance
What is AI technical title?
AI technical title is built by PatSnap AI team. It summarizes the technical point description of the patent document.
A technology of amlodipine aspartate and a synthesis method, which is applied in the field of amlodipine aspartate compound and its synthesis, can solve the problems of high production risk, low total yield, complicated process and the like, and achieves less toxic and side effects , the route is short, the effect of improving the compliance
CN102718698BActive 📅 Publication Date: 2013-11-20ZHEJIANG JIANFENG PHARM CO LTD
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Embodiment 1
[0036] The specific implementation manner of the present invention will be described in detail below in conjunction with the accompanying drawings.
[0037] 1.1 Preparation of amlodipine (such as figure 1 shown):
[0038] 1.1.1 Reaction formula:
[0039]
[0040] 1.1.2. Material ratio:
[0041] Material name Feeding amount moles amlodipine imide 20kg 36.6 Hydrazine hydrate 3.3kg 55.7 Absolute ethanol 150kg
[0042] 1.1.3. Operation process:
[0043] Add 20kg of amlodipine imine, 150kg of absolute ethanol, and 3.3kg of hydrazine hydrate into the reaction kettle, heat up and reflux for 2 hours (TLC detects the end point of the reaction), cool to room temperature, filter, and the filter cake is washed with a small amount of absolute ethanol, and the filtrate is reduced Concentrate to dryness under pressure, add 140kg of dichloromethane to the residue, stir to dissolve, wash with 50kg of water, and then wash once with 30kg of...
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Abstract
The invention relates to the field of medicine, and in particular relates to an aspartic acid amlodipine compound and a synthesis method thereof. The aspartic acid amlodipine compound has the structural formula shown in the specification. The aspartic acid amlodipine series salt is suitable for hypertensives with various complications such as diabetes mellitus, stenocardia, asthma and peripheral arterial diseases, and can be used for effectively reducing the left ventricular mass index (LVMI) and reverse left ventricular hypertrophy as well as blood vessel structure change caused by hypertension; the aspartic acid amlodipine compound has durable action and mild effect without improving the preparation, and has no drug accumulation; and the aspartic acid amlodipine compound has the characteristics of being less in toxic and side effects and endurable for patients and improving the compliance of the patients. Furthermore, the compound is lower in cost.
Description
technical field [0001] The invention relates to the field of medicine, in particular to an amlodipine aspartate compound and a synthesis method thereof. Background technique [0002] Amlodipine (Amlodpine) [0003] English chemical name: [0004] 3-ethyl(±)2[(2-aminoethoxy)methyl]-4-(2-chlorophenyl) [0005] -3.5-pyridine di-carbonylate [0006] Chinese chemical name: 3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2chlorophenyl)-1.4-dihydro-6-methyl-3.5-pyridinedicarboxylate Ester [0007] Structural formula: [0008] [0009] Molecular formula: C 20 h 25 N 2 o 5 Cl [0010] Molecular weight: 409.1 [0011] Amlodipine is a long-acting calcium influx blocker, which blocks extracellular calcium ions in myocardial and vascular smooth muscle cells from entering cells through calcium ion channels in the cell membrane, directly relaxes vascular smooth muscle, expands peripheral arterioles, dilates coronary arteries, and relieves coronary artery disease. The role of art...
Claims
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