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Mar. 31th 2025
Medetomidine Hydrochloride is a customized product of our laboratory. Our researchers have been engaged in the industry for more than 10 years and have rich experience in the customization of chemicals. Our company engaged in the chemical industry for 15 years, has a good reputation and productivity. The chemical formula of it is C13H17ClN2, which is an organic compound. It is a white to almost white crystalline powder with a special odor. It is stable at room temperature and easily soluble in water, but its solubility is low in organic solvents. Relatively stable at high temperatures, but decomposition may occur under extreme conditions. Easily soluble in polar solvents such as water, methanol, and ethanol, and slightly soluble or insoluble in a few non polar solvents. It is a hydrochloride and therefore has acidity in water. It can react with alkali to generate corresponding salts. It is a chiral compound with two Enantiomer. It is a compound with optical activity. Specific rotation of ([ α] D) Usually reported at specific measurement wavelengths and conditions, it can be used to characterize the optical rotation properties of compounds.
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Melting point |
164-166 ° C |
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Storage conditions |
Inert atmosphere |
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Store in freezer |
under − 20 °C |
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Steam pressure |
1.08E − 05mmHg at 25 °C |
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LogP |
3.98030 |
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PSA |
28.68000 |
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Precision mass |
236.10800 |
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In anesthetized rats, medetomidine ( 1–100 ug / kg, intravenous injection ) caused a short dose-dependent decrease in blood pressure and heart rate. Medetomidine showed potent vasopressor effect ( PD501.7μg / kg ) and sympathetic inhibitory effect ( ID501.6μg / kg ) in rats with encephalomyelitis, without affecting the basal heart rate of Chemicalbook. Medetomidine induced dose-dependent sedation, induced loss of positive reflex and decreased body temperature at high doses ( > 100 ug / kg ). Medetomidine decreased the turnover rate of biogenic amines in the brain. Medetomidine inhibited turnover in a dose-dependent manner, and inhibited dopamine turnover and serotonin turnover in the brain at high doses.
1. Muscle relaxants:
Because of its muscle relaxation effect, it can be used as a Muscle relaxant in some cases. For example, during animal surgery, its muscle relaxation function helps to make surgical instruments easier to insert and operate.
2. Sleep suppressants:
Can be used to help animals or humans fall asleep. Its sedative and analgesic effects make it a choice for the treatment of insomnia, anxiety and other Sleep disorder. Due to its strong sedative effect and rapid onset, it is commonly used for short-term and temporary sleep assistance therapy.
Medetomidine Hydrochloride is a high selective, high specific and high strength α Adrenergic receptor agonists are mainly used for sedation, analgesia, inhibition of stress response and maintenance of hemodynamic stability in intensive care patients during surgery. Among the synthesis routes of metomidine reported in the literature at present, one part needs to protect imines, which has many steps, large reagent consumption and high cost. The other part has harsh reaction conditions and needs to use more dangerous reagents in the process. Therefore, it is necessary to improve the synthesis method for its key intermediates. The key intermediate 2- (2,3-xylenyl) - 2-methylethylene oxide was prepared by the reaction of (CH3) 3s+hso4- with 1- (2,3-dimethylphenyl) ethanone. The reaction conditions of carbonyl epoxidation were optimized by simplex optimization method. The optimal epoxidation conditions were obtained as follows: material ratio nkoh:n1 (2,3-xylenyl) ethane = 18.43:1.00, n methanol: n1- (2,3-xylenyl) ethane =2.2:1.0, reaction temperature 39 ℃, reaction time 7.45h, The epoxidation yield was 60.1%.
Starting from the starting material 2,3-dimethylphenylethylamine, Medetomidine Hydrochloride is synthesized through a series of chemical transformations.
The steps are described as follows:
Purpose: To protect the amino group of 2,3-dimethylphenylethylamine for subsequent functional group conversion.
R-NH2 + R'COCl → R-NHCOOR' + HCl
(Where R=2,3-dimethylphenethyl, R '=acetyl or other acyl)
In practical operation, acetyl chloride (R'COCl=CH3COCl) is commonly used as an acylation reagent, which reacts with 2,3-dimethylphenylethylamine under acidic conditions (such as using pyridine and aluminum trichloride as catalysts) to generate N-acetyl-2,3-dimethylphenylethylamine (i.e. R-NHCOCH3). However, please note that the catalysts and conditions used here may vary depending on specific experiments.
Objective: To convert the acylation product into alkyl nitrite as an intermediate for subsequent reactions.
Note: The specific reaction mechanism of this step may vary depending on the selected reagents and conditions. The following is a simplified hypothetical reaction.
R-NHCOOR '+(CH3) 3SO4+NaNO2 → R-N (O) OCH3+byproduct
(Among them, R-NHCOOR 'is the first step product, and (CH3) 3SO4 is trimethyl sulfate)
Objective: To reduce alkyl nitrite esters to imines in preparation for the subsequent introduction of functional groups.
R-N(O)OCH3 + H2 → R-CH=NR' + H2O + CH3OH
(In the presence of catalysts such as palladium carbon)
However, please note that the above equation is a simplified representation, and in reality, the hydrogenation reduction of nitrite esters may be more complex and may not necessarily directly generate imines. It is more likely that nitrite esters first decompose into the corresponding alcohols and nitrogen oxides, and then the alcohols are oxidized (or imines are directly generated from other pathways), and finally imines are obtained through reduction. However, in order to maintain the simplicity of the explanation, we directly provide a hypothetical transition from nitrite ester to imine here.
Objective: To construct the precursor compound of metoclopramide by introducing the desired functional groups through acylation or other reactions based on imine.
R-CH=NR' + R''COCl → R-CH(NR'COR'')-R''' + HCl
(Among them, R '', R '' 'represents the introduced functional groups and side chains)
In fact, this step may involve multiple reactions, including acylation, alkylation, cyclization, etc., to construct precursor compounds with specific structures and activities. The specific conditions and reagents for these reactions will depend on the specific structure of the target compound.
Objective: To convert the precursor compound into its hydrochloride form and obtain high-purity metoclopramide hydrochloride through purification steps.
R-CH (NR'COR '') - R ''+HCl → [R-CH (NR'COR '') - R ''] Cl · HCl+solvent
(Conducted in appropriate solvents such as ethanol or water)
Then, through purification steps such as crystallization, filtration, washing, and drying, crystals of metoclopramide hydrochloride are separated from the reaction mixture. These steps typically involve solvent selection, temperature control, and possible recrystallization processes to improve product purity and yield. The specific laboratory synthesis methods and operating conditions can be found in relevant scientific literature. If you have specific needs, it is recommended to consult a chemical expert or refer to synthesis literature for a detailed description of the compound's synthesis method. At the same time, when conducting chemical synthesis experiments, relevant laboratory safety operating procedures should be followed, and appropriate laws and regulations should be followed.
What are the side effects of this compound?
1.Cardiovascular system response
hypotension
It is one of its most common side effects, and its incidence may be high. This may be due to the direct effect of drugs on vascular smooth muscle or their regulation of cardiovascular function by affecting the central nervous system.
bradycardia
It can inhibit the cardiac conduction system, leading to a decrease in heart rate. This side effect may be more significant in elderly patients or those with poor heart function.
sinus arrest
In some cases, it may cause sinus rhythm arrest, which is a serious arrhythmia.
transient hypertension
Although not as common as hypotension, there are also reports indicating that in some patients, it may cause an increase in blood pressure.
2.Neurological response
- Dry mouth: It is one of its common neurological side effects, which may be related to the inhibition of oral saliva secretion by drugs.
- Neuromuscular blockade: Although it is unlikely to cause significant neuromuscular blockade at regular doses, attention should still be paid to its potential neuromuscular blockade effects when administered at high concentrations or rapidly.
3.Other reactions
Gastrointestinal reactions
Nausea, vomiting, etc. may be related to their direct impact on the smooth muscles of the gastrointestinal tract.
Respiratory depression
In some cases, Medetomidine Hydrochloride may cause a decrease in respiratory rate and depth, especially when the drug dosage is too high or the patient has underlying respiratory disease.
Allergic reaction
Patients who are allergic to it or its components may experience allergic reactions such as rash, itching, difficulty breathing, etc. Therefore, the patient's allergy history should be carefully inquired before use.
4.Special population reactions
Patients with renal dysfunction
Due to the fact that the compound is mainly excreted through the kidneys, the drug may accumulate in the body in patients with renal impairment, increasing the risk of adverse reactions.
Elderly patients
The cardiovascular system of elderly patients is more sensitive to drugs, so special attention should be paid to monitoring their cardiovascular system response when using it.
5.precautions
- It should be used by professionals with medical monitoring equipment.
- Continuous monitoring, especially of the cardiovascular system, should be conducted during use.
- If adverse reactions occur, the medication should be stopped immediately and necessary treatment measures should be taken.
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