Synthesis method of amlodipine free alkali

The technology of a kind of amlodipine, synthetic method is applied in the synthesis field of amlodipine free base, can solve the problems such as easy explosion, increase production, safety facility and environmental protection treatment cost, achieve yield improvement, reaction time reduction, economy Improved effect

Inactive Publication Date: 2015-01-07
CHANGZHOU RUIMING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] In the above-mentioned method of using phthaloyl amlodipine and 80% aqueous solution of hydrazine hydrate to react, the use of toxic and explosive aqueous solution of hydrazine hydrate will significantly increase production, safety facilities and environmental protection treatment costs

Method used

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  • Synthesis method of amlodipine free alkali
  • Synthesis method of amlodipine free alkali

Examples

Experimental program
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Effect test

Embodiment 1

[0022] Put 420kg of 5% sodium hydroxide aqueous solution and 130kg of disodium phthalate into the reaction kettle after weighing, start stirring, react at room temperature for 6 hours, put them into a centrifuge, wash with water to remove disodium phthalate, and obtain ammonia Clodipine (base) 100kg, yield 93.5%, content more than 99%.

Embodiment 2

[0024] Weigh 440kg of 5% sodium hydroxide aqueous solution and 120kg of disodium phthalate and put them into the reaction kettle, start stirring, react at room temperature for 5 hours, put them into a centrifuge, wash with water to remove disodium phthalate, and obtain ammonia Clodipine (base) 95kg, yield 92.3%, content more than 99%.

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Abstract

The invention relates to a synthesis method of amlodipine free alkali. According to the synthesis method of the amlodipine free alkali, phthaloyl amlodipine is used as a raw material and is hydrolyzed by a sodium hydroxide aqueous solution under the condition of room temperature to prepare the amlodipine free alkali. By virtue of the synthesis method of the amlodipine free alkali, the 5% sodium hydroxide aqueous solution is used as a reaction solution, so that the economy is obviously improved; the synthesis method of the amlodipine free alkali is relatively environmental friendly and stable; the economy is improved; the yield is obviously improved.

Description

technical field [0001] The invention relates to the field of chemical industry and pharmacy, in particular to a method for synthesizing amlodipine free base. Background technique [0002] Amlodipine (base), chemical name: (±)-2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-3-ethoxycarboxy-5-methoxycarboxy-6- Methyl-1,4-dihydropyridine, [0003] The structural formula is as follows: [0004] [0005] Amlodipine (base) and benzenesulfonic acid, hydrochloric acid, maleic acid and other acids after the salt formation of drugs are dihydropyridine calcium antagonists (calcium ion antagonists or slow channel blockers). Calcium antagonists, also known as calcium channel blockers, are first-line basic antihypertensive drugs and are widely used in clinical practice. There are many types of calcium antagonists, and their pharmacokinetics and pharmacodynamics characteristics are obviously different. The chemical structure of amlodipine is similar to that of nifedipine, but it has uniq...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90
CPCC07D211/90
Inventor 史卫明
Owner CHANGZHOU RUIMING PHARMA
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