Aspartic acid amlodipine compound and synthesis method thereof

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...

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Problems solved by technology

[0013] Existing amlodipine promptly takes chloroethanol as starting raw material, reacts with sodium azide to generate azide ethanol, then condenses with ethyl chloroacetoacetate to generate azide ester under the action of sodium hydride, azide ester and 2-chloro The Hantzsch cyclization reaction between benzaldehyde and methyl β-aminocrotonate produces a cyclic compound, and the cyclic compound is formed on Pd / CaCO 3 Amlodipine is produced by reduction reaction with hydrogen under catalysis. The original process uses chloroethanol as the starting material, and materials such as explosive and highly toxic sodium azide are used in the production. The production is dangerous, and the steps are long, the process is complicated, and the total Low yield (only 13%)

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