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Preparation method of bisoprolol fumarate impurity

A technology for bisoprolol fumarate and impurities, applied in the field of preparation of bisoprolol fumarate impurities

Pending Publication Date: 2021-03-05
深圳市祥根生物科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, there is no literature report on the preparation method of this compound

Method used

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  • Preparation method of bisoprolol fumarate impurity
  • Preparation method of bisoprolol fumarate impurity

Examples

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Embodiment 1

[0024] A preparation method for bisoprolol fumarate impurity, comprising the following steps:

[0025] Preparation of compound Ⅰ: Dissolve p-hydroxybenzaldehyde (12.40g, 100.00mmol) in N,N-dimethylformamide (100mL), add potassium carbonate (27.60g, 200.00mmol), then add 3-bromo Propylene (13.30g, 110.00mmol), stirred at room temperature for 2h. The reaction solution was filtered, water (500ml) and ethyl acetate (200ml×3) were added to the filtrate for extraction, the organic phase was dried over anhydrous sodium sulfate, and concentrated under reduced pressure to obtain 16.20g of crude compound II. It was directly used in the next step without purification.

[0026] Preparation of compound II: Dissolve compound I (16.20g, 100.00mmol) in methanol (100ml), add sodium borohydride (7.60g, 200.00mmol) in batches at 0°C, react at 0°C for 2h, and slowly heat up to At room temperature, the reaction was continued for 4h. Concentrate under reduced pressure, add saturated aqueous ammo...

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Abstract

The invention discloses a preparation method of a bisoprolol fumarate impurity. The preparation method comprises the following steps: with p-hydroxybenzaldehyde as a raw material, carrying out six-step reactions to synthesize the impurity. The method has the advantages of reasonable synthesis route design, simple post-treatment, mild reaction conditions, good operability and usage of cheap and easily available raw materials. The bisoprolol fumarate impurity prepared by using the method disclosed by the invention provides an important basis for quality control, safety and effectiveness evaluation of bisoprolol fumarate, and has an important application value.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a preparation method of bisoprolol fumarate impurity. Background technique [0002] Bisoprolol Fumarate is a white crystalline powder, its chemical name is 1-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy-3 -(1-methylethyl)amino-2-propanol fumarate is a selective β1 receptor blocker without intrinsic sympathomimetic and membrane stabilizing activity. It is clinically used to treat cardiovascular diseases such as hypertension, angina pectoris and arrhythmia. It has definite curative effect, few side effects, and long drug half-life, so patients only need to take medicine once a day. It has obvious advantages and broad application prospects in drugs with the same target. [0003] It is well known that for human drug use, domestic and international regulatory agencies set very low limits for unidentified or undetermined toxicity impurities in APIs, usually less than 0.1% b...

Claims

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Application Information

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IPC IPC(8): C07C213/04C07C217/34C07D301/14C07D303/23C07C41/16C07C43/205C07C41/01C07C43/12C07C41/26C07C43/23C07C45/64C07C47/575
CPCC07C41/01C07C41/16C07C41/26C07C45/64C07C213/04C07D301/14C07D303/23C07C47/575C07C43/23C07C43/126C07C43/2055C07C217/34
Inventor 孙坤杰
Owner 深圳市祥根生物科技有限公司
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