Preparation method of terbutaline sulfate

A technology of terbutaline sulfate and compound, applied in the field of medicine, can solve the problems of long steps, low yield, large environmental pollution, etc., and achieve the effects of low production cost, easy availability of materials, and low equipment requirements

Inactive Publication Date: 2021-06-29
北京睿悦生物医药科技有限公司 +1
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Problems solved by technology

[0009] Aiming at the technical problems of using high-risk and highly toxic reagents, long steps, low yield and great environmental pollution in the synthesis process of terbutaline sulfate existing in the prior art, the purpose of the present invention is to provide a kind of terbutaline sulfate The preparation method of Lin shortens the reaction steps and improves the yield while reducing environmental pollution and production costs

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  • Preparation method of terbutaline sulfate
  • Preparation method of terbutaline sulfate
  • Preparation method of terbutaline sulfate

Examples

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Embodiment 1

[0033] This example provides a preparation method of terbutaline sulfate, using 3,5-dihydroxyacetophenone as a raw material, through oxidation reaction, condensation reaction, carbonyl reduction reaction, and sulfuric acid salt formation, to obtain terbutaline sulfate Lin includes the following methods:

[0034] Step 1, oxidation reaction:

[0035] 50.0g (0.33mol) of 3,5-dihydroxyacetophenone was dissolved in 400ml DMSO, and 112ml of hydrobromic acid (HBr) (0.99mol) with a mass concentration of 48% was added at 30°C to 40°C to keep The temperature was reacted for 13 to 16 hours, and after it was lowered to room temperature, it was added to ice water, extracted with an organic solvent including dichloromethane, and the organic phase was concentrated under reduced pressure to dryness to obtain a solid, which was 3,5 as shown in formula (I). -44.54 grams of dihydroxyphenylglyoxal, and the molar yield reaches 73.3%.

[0036]

[0037] Step 2, condensation reaction:

[0038] T...

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Abstract

The invention provides a preparation method of terbutaline sulfate. The preparation method comprises the following steps: with 3,5-dihydroxyacetophenone as a raw material, directly carrying out an oxidation reaction on 3,5-dihydroxyacetophenone without protecting a phenolic hydroxyl group so as to obtain aromatic glyoxal, and then carrying out a condensation reaction, a reduction reaction and sulfuric acid salification on the aromatic glyoxal and tert-butylamine to obtain terbutaline sulfate. According to the method, a high-risk operation unit for hydrogenation debenzylation in an existing terbutaline sulfate preparation process is eliminated; and meanwhile, bromination reaction with relatively large pollution to the environment is avoided, and the whole process is more suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a preparation method of terbutaline sulfate. Background technique [0002] Terbutaline Sulfate, also known as hydroxyalbutaline and terbutaline, was first developed by AstraZeneca Pharmaceuticals Co., Ltd. and was produced and marketed abroad in 1988. Clinically, it is mainly used for the treatment of bronchospasm in bronchial asthma, asthmatic bronchitis and chronic obstructive pulmonary disease. The published processes for preparing terbutaline sulfate all have the problems of long routes, unsatisfactory atomic economics, serious environmental pollution, highly toxic raw materials and dangerous operating units involved in production, and are not suitable for industrial production. Common preparation processes The details are as follows: [0003] Route 1: The route adopted by the patent US3937838 of the original manufacturer AstraZeneca Pharmaceuticals Co., Ltd.: 3,5-dihydrox...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C213/00C07C213/08C07C215/30
CPCC07C213/00C07C213/08C07C249/02C07C45/28C07C215/30C07C251/16C07C49/86
Inventor 陈亮付冀峰宛六一
Owner 北京睿悦生物医药科技有限公司
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