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Preparation method of ambroxol hydrochloride impurity F

A technology for ambroxol hydrochloride and impurities, which is applied in the field of medicinal chemistry, can solve problems such as difficult control of reaction conditions, and achieve the effects of mild reaction conditions, high yield, and simple operation

Pending Publication Date: 2021-11-05
重庆健能医药开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The existing literature Journal oflabeled compounds and radiopharmaceuticals; Vol.53; nb.1; (2010); P.15-23 and patents (CN109810066 and CN110551071) all adopt condensation, oxidation two-step method to carry out the synthesis of this compound, use in the reaction Formaldehyde and ammonium cerium nitrate, the reaction conditions are not easy to control

Method used

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  • Preparation method of ambroxol hydrochloride impurity F
  • Preparation method of ambroxol hydrochloride impurity F
  • Preparation method of ambroxol hydrochloride impurity F

Examples

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Effect test

Embodiment 1

[0030] 4-(6,8-dibromo)-3,4-dihydroquinazolin-3-yl)-cyclohexanol (impurity F)

[0031] Add 40 g of ambroxol hydrochloride and 400 g of formic acid into the reaction bottle, heat at 80° C. to 90° C. for 4-6 hours, and TLC detects that the reaction is complete. Remove formic acid by rotary evaporation at 80°C to 90°C, then add 500ml of dichloromethane and 200ml of water, adjust the pH to 8-9 with saturated sodium carbonate solution, let stand to separate the liquids, dry the organic phase with anhydrous sodium sulfate, and spin to dry the solvent A solid was obtained, weighing 34.9 g, with a yield of 93.2%.

[0032] Example 1

[0033] 4-(6,8-dibromo)-3,4-dihydroquinazolin-3-yl)-cyclohexanol (impurity F)

[0034] Add 40 g of ambroxol hydrochloride and 160 g of formic acid into the reaction flask, heat at 60° C. to 70° C. for 4-6 hours, and TLC detects that the reaction is complete. Remove formic acid by rotary evaporation at 80°C to 90°C, then add 500ml of dichloromethane and 2...

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Abstract

The invention provides a preparation method of an ambroxol hydrochloride impurity F. The ambroxol hydrochloride impurity F is prepared by a condensation reaction, and the chemical equation is shown in the specification. The method is simple to operate and high in yield. No special equipment is needed, and reaction conditions are mild.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, in particular to a preparation method of ambroxol hydrochloride impurity F. Background technique [0002] Ambroxol hydrochloride, chemical name trans-4-[(2-amino-3,5-dibromobenzyl) amino]-cyclohexanol hydrochloride, chemical structural formula is formula (I) compound. [0003] [0004] Ambroxol hydrochloride is an expectorant, commonly used in acute and chronic lung diseases accompanied by abnormal sputum secretion and poor expectoration function. It was listed in Germany in the early 1980s. The drug is a non-patent drug. After consulting and researching the existing pharmacopoeia standards, there is an impurity 4-(6,8-dibromo)-3,4-dihydroquinazolin-3-yl)-ring Hexanol (impurity F), its structural formula is shown in formula (F): [0005] [0006] The existing literature Journal oflabeled compounds and radiopharmaceuticals; Vol.53; nb.1; (2010); P.15-23 and patents (CN109810066 and CN110...

Claims

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Application Information

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IPC IPC(8): C07D239/74
CPCC07D239/74
Inventor 蔡鹏飞叶世春王雪
Owner 重庆健能医药开发有限公司
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