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Bisoprolol powder is a highly selective β₁-adrenergic receptor blocker. Its chemical name is (±)-1-[4-[[2-(1-methyl ethoxy) ethoxy] methyl] phenoxy]-3-[(1-methyl ethyl)amino]-2-propanol. The molecular formula is C₁₈H₃₁NO₄. It appears as a white to off-white crystalline powder, which is slightly soluble in water and readily soluble in organic solvents such as methanol or ethanol.
As a raw material for cardiovascular drugs, Bisoprolol inhibits sympathetic nerve activity, reduces myocardial contractility and heart rate, and is used to treat hypertension, angina pectoris and chronic heart failure. Its high β₁-selectivity reduces the impact on β₂ receptors and lowers the risk of side effects such as bronchospasm. The raw material needs to strictly meet GMP standards to ensure purity and stability. It is often further processed into tablets or capsules. Storage should be protected from light and moisture, and kept in a cool and dry place.
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Chemical Formula |
C18H31NO4 |
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Exact Mass |
325 |
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Molecular Weight |
325 |
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m/z |
325 (100.0%), 326 (19.5%), 327 (1.8%) |
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Elemental Analysis |
C, 66.43; H, 9.60; N, 4.30; O, 19.66 |
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Bisoprolol, or bisoprolol fumarate, is a widely used drug primarily used to treat a variety of cardiovascular diseases. Its main uses and characteristics can be summarized as follows:
main purpose
Hypertension
Bisoprolol Powder is a beta-blocker that selectively blocks the connection between epinephrine and beta1 receptors, thereby lowering blood pressure. This drug can be used alone or in combination with other antihypertensive drugs to achieve better blood pressure control.
Coronary heart disease (angina pectoris)
By blocking cardiac β1 receptors, Bisoprolol can reduce myocardial oxygen consumption and increase coronary blood flow, thereby alleviating angina symptoms. It is a commonly used treatment for patients with coronary heart disease.
Myocardial infarction
Studies have shown that treatment with beta-blockers (such as Bisoprolol) after myocardial infarction can significantly improve the survival rate of patients. This is mainly attributed to its antiarrhythmic and anti-ischemic effects, as well as a possible reduced platelet aggregation capacity.
Arrhythmia
Bisoprolol is also used to treat a variety of cardiac arrhythmias, such as supraventricular tachycardia, atrial fibrillation, and premature ventricular contractions. It helps restore the normal rhythm of the heart by regulating the electrophysiological activity of the heart.
Drug properties
High selectivity
Bisoprolol has high affinity and selectivity for cardiac β1 receptors and has less effect on β2 receptors of bronchial and vascular smooth muscles, so it causes less respiratory side effects during use.
Long-term effect
The drug is rapidly and completely absorbed after oral administration. The effect of one dose can last for 24 hours, making it convenient for patients to use.
Safety
Bisoprolol has no cell membrane stabilizing effect within the therapeutic dose range and has no adverse effects on blood sugar and blood lipids. Therefore, it is safe to use in patients with diabetes.
Warning word, Hazard description H302, Dangerous goods sign xn, Hazard category code 22, WGK Germany 1, RTECS No. ub8380000, HazardClass IRRITANT
Pharmacological action of bisoprolol: bisoprolol is selective β 1 adrenoceptor blockers, within the therapeutic dose range, have no obvious membrane stabilizing effect or intrinsic sympathetic effect. However, its cardiac selectivity is not absolute, and it is also inhibited at high dose (≥ 20mg) β 2 adrenoceptors, mainly located in bronchial and vascular smooth muscle; To maintain selectivity, it is particularly necessary to use the lowest effective dose. yes β The selectivity of 1 receptor is 4 times that of atenolol. Bisolol's β 1 receptor blockade is the main effect of reducing blood pressure.
Bisoprolol Powder is a new generation of selectivity β 1-adrenergic receptor blocker, without intrinsic sympathetic activity and membrane stabilization, has an inhibitory effect on renin secretion. Almost all of them are absorbed by oral administration, with a bioavailability of over 90% and a half-life of 10-12 hours. A single administration can maintain the efficacy for 24 hours, and long-term use has no cumulative toxicity. It also has lipophilicity β- Adrenergic receptor blockers have fast absorption and hydrophilicity β- Adrenergic receptor blockers have the advantages of long half-life and low first-pass effects. They have a 50% metabolic rate in both liver and kidney, and can be used even in cases of liver and kidney dysfunction. Another advantage is that there are minimal differences in pharmacokinetics between individuals of different genders, ages, and individuals, making it easy to master clinically. Bisoprolol fumarate has high selectivity for β Affinity ratio of 1 receptor β 2 receptors are 11-34 times stronger, with the strongest compared to atenolol and metoprolol β 1 receptor selective inhibitory effect.
We can supply Bisoprolol Powder.
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Using p-hydroxybenzaldehyde (compound I) as the starting material and following the steps you described, bisoprolol free base can be prepared.
1. Reduction to obtain p-hydroxybenzyl alcohol (compound ii)
C7H6O2+reducing agent → C7H8O2
By using reducing agents such as hydrogen or phosphite, p-hydroxybenzaldehyde is reduced to p-hydroxybenzyl alcohol. This step reduces the aldehyde functional group to an alcohol functional group.
2. Etherification with isopropoxyethanol to obtain compound III
C7H8O2+C5H12O2+acid catalyst → product of ether formation with isopropoxyethanol (compound III)
React p-hydroxybenzyl alcohol with isopropoxyethanol (etherification of isopropanol and ethylene glycol) to produce compound III. This reaction generally requires acidic conditions, and the commonly used catalyst is sulfuric acid.
3. Etherification with epichlorohydrin to obtain compound IV
Compound III+C3H5ClO+alkali catalyst → product of ether formation with epichlorohydrin (Compound IV)
React compound III with epichlorohydrin to form compound IV. In this reaction, epichlorohydrin opens the ring and undergoes a substitution reaction with the ether functional group. This step requires alkaline conditions, and alkaline catalysts such as sodium hydroxide or sodium carbonate can be selected.
4. Ring opening reaction with isopropylamine to obtain bisoprolol free base
Compound IV+C3H9N → Bisoprolol free base
Compound IV undergoes a ring opening reaction with isopropylamine to form a bisoprolol free base. In this step, the epoxy group is attacked by isopropylamine, generating the final bisoprolol free base.
Bisoprolol Powder was synthesized from 4 - hydroxybenzyl alcohol and isopropyl alcohol, epichlorohydrin, isopropylamine and fumaric acid in four steps. For the complex first step reaction, the acid-base treatment method was used to obtain the product, so as to avoid the high temperature and high vacuum distillation method, which not only greatly improved the yield, but also greatly reduced the reaction energy consumption. The structure of the product was characterized by liquid chromatography, melting point, Fourier transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. This synthetic method has the advantages of mild conditions, simple post-processing operation and high product yield, which can be industrialized.
The main pathway of action of bisoprolol in the body involves regulation of the cardiovascular system. As a selective beta 1 receptor blocker, it exerts its therapeutic effects in the body through specific mechanisms. The following is a detailed explanation of the mechanism of action of Sorol in vivo:
Mechanism of action
Bisoprolol mainly exerts its effects by blocking β 1 receptors on the membrane of smooth muscle cells in the heart and blood vessels. These receptors are a type of adrenergic receptor that, when adrenaline binds to them, triggers physiological responses such as cardiac contraction, increased heart rate, and vasoconstriction. After binding to these receptors, bisoprolol can block the activation of adrenaline, thereby reducing myocardial contractility, heart rate, and blood pressure.
Specific pathways of action
Lowering blood pressure:
Bisoprolol reduces myocardial contractility and heart rate by blocking β 1 receptors, thereby lowering cardiac output and reducing peripheral vascular resistance, resulting in a steady decrease in blood pressure. This effect is particularly important for patients with hypertension, as it can effectively control blood pressure levels and reduce the occurrence of cardiovascular events.
Improve heart function:
Bisoprolol can reduce myocardial oxygen consumption, improve myocardial ischemia, and alleviate symptoms of angina pectoris. In the treatment of coronary heart disease, it helps stabilize the condition and improve the quality of life of patients. In addition, bisoprolol also has the effect of inhibiting cardiac remodeling, maintaining the normal structure and function of the heart, and reducing the mortality rate of heart failure patients.
Antiarrhythmic treatment:
Bisoprolol reduces the occurrence of arrhythmia by regulating the electrophysiological activity of the heart. This effect is particularly important in patients with arrhythmia, as it can reduce complications and mortality caused by arrhythmia.
Central inhibitory effect:
Bisoprolol also has a certain central inhibitory effect, which can suppress the excitability of the sympathetic nervous system, thereby achieving the effect of calming the nerves. This effect helps alleviate patients' tension and anxiety, and improve sleep quality.
Anti-inflammatory effect:
In some cases, bisoprolol also has certain anti-inflammatory effects. When the body is infected with bacteria or viruses, local inflammation may occur. Bisoprolol can inhibit the release of inflammatory mediators, alleviate inflammatory reactions, and thus help with disease recovery.
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