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Trimebutine is a smooth muscle regulator acting on the gastrointestinal tract. Its pharmacological mechanism is unique and complex, mainly exerting its efficacy through dual regulatory actions: it can simultaneously activate peripheral opioid receptors (μ, κ, and δ receptors) and block sodium ion channels, thereby comprehensively regulating intestinal motility. This effect enables it to intelligently exert opposite effects according to the different states of the intestine - it can relax and relieve spastic intestines when they are in a contracted state, and enhance the contraction activity of intestines with insufficient tension when they are in a relaxed state, ultimately restoring the normal rhythm of the disordered gastrointestinal tract. It is hailed as the "regulator of gastrointestinal rhythm". Clinically, it is widely used to treat various functional gastrointestinal disorders, such as abdominal pain, abdominal distension, and changes in defecation habits (alternating diarrhea and constipation) caused by irritable bowel syndrome (IBS), as well as functional dyspepsia symptoms. This drug usually has good tolerance, and common dosage forms include tablets and triametaphenoxidine maleate granules. It is a core therapeutic drug that addresses functional disorders from the functional level of motility.

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Chemical Formula |
22H29NO5 |
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Exact Mass |
387 |
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Molecular Weight |
387 |
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m/z |
387 (100.0%), 388 (23.8%), 389 (2.7%), 389 (1.0%) |
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Elemental Analysis |
C, 68.20; H, 7.54; N, 3.61; O, 20.65 |

Trimebutine, as a gastrointestinal antispasmodic drug, has a wide range of applications and is important, mainly used to treat various symptoms related to gastrointestinal dysfunction.
Gastrointestinal symptoms caused by chronic gastritis: It has a significant relieving effect on common gastrointestinal symptoms in patients with chronic gastritis, such as abdominal distension, abdominal pain, belching, etc. It can alleviate these symptoms by regulating the contraction and relaxation of gastrointestinal smooth muscles, improving gastric motility, promoting gastric emptying.
Irritable bowel syndrome: Irritable bowel syndrome is a functional intestinal disease, often characterized by abdominal pain, diarrhea, constipation, or alternating symptoms. The treatment effect of irritable bowel syndrome is significant, which can regulate intestinal motility, relieve abdominal pain, improve diarrhea and constipation symptoms, and enhance the quality of life of patients.


Postoperative recovery of intestinal function: After abdominal surgery, it often takes some time for the patient's intestinal function to recover. It can promote the peristalsis of intestinal smooth muscle, accelerate the recovery of intestinal function, and reduce the occurrence of postoperative intestinal complications.
Barium enema examination: During barium enema examination, it can accelerate the flow of barium in the intestine, thereby shortening the examination time and improving the examination efficiency.
The mechanism of action is complex and diverse, mainly including the following aspects:
Regulating gastrointestinal motility
It can directly act on the smooth muscles of the gastrointestinal tract by inhibiting the permeability of K+, acting on adrenergic receptors, inhibiting the permeability of Ca2+, and acting on cholinergic K receptors through various pathways, regulating the contraction and relaxation of gastrointestinal smooth muscles and improving gastrointestinal motility function.
Improving gut microbiota
Although it does not directly affect the gut microbiota itself, it helps promote the growth of beneficial bacteria and inhibit the proliferation of harmful bacteria by improving gastrointestinal motility, thereby improving the gut environment and alleviating gastrointestinal discomfort symptoms.
Protecting the gastrointestinal mucosa
It can reduce gastrointestinal irritation, protect the gastrointestinal mucosa, and prevent further damage. This is of great significance for alleviating gastrointestinal inflammation and promoting the repair of gastrointestinal mucosa.
Gastrointestinal pain relief
It also has the function of gastrointestinal pain relief. It can alleviate symptoms of abdominal pain by stimulating peripheral opioid receptors, releasing active substances such as gastrointestinal peptides and gastrin.

The synthesis of Trimebutine mainly consists of three steps
Step 1:
Under the action of a catalyst, the compound 2-amino-2-phenylbutyric acid of formula II is reduced by borohydride in an organic solvent to obtain the intermediate compound 2-amino-2-phenylbutanol;
Step 2:
Perform amine methylation reaction on compound 2-amino-2-phenylbutanol, formaldehyde, and formic acid of formula III to obtain intermediate formula IV compound 2- (dimethylamino) -2-phenylbutanol;
Finally:
In the presence of an acid binding agent, the raw material compound V, 3,4,5-trimethoxybenzoyl chloride, is esterified with the intermediate compound IV, 2- (dimethylamino) -2-phenylbutanol, to obtain the final product.
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The specific steps are as follows:
134.3g of solvent tetrahydrofuran is added to a clean four necked flask, stirring is started, and 17.9g (0.1mol) of raw materials 2-amino-2-phenylbutyric acid and 8.3g (0.22mol) of sodium borohydride are sequentially added. Then, the system temperature is controlled at 10-20 ℃ while stirring, and 12.7g (0.13mol) of sulfuric acid is slowly added dropwise. After the dropwise addition is completed, the reaction is kept at room temperature for 12 hours. During the reaction process, a central control sample can be taken. After the central control is qualified, the system temperature of the reaction solution is cooled to 10 ℃, and 53.7g (0.27mol) of a 20% sodium hydroxide aqueous solution is added dropwise. The dropwise addition temperature is controlled at 10-15 ℃. After the dropwise addition is complete at ℃, heat up to reflux for 2 hours, stop heating and let it stand for layering. Collect the upper organic phase and concentrate it under reduced pressure to recover tetrahydrofuran, 14.2 g of the intermediate product formula III compound 2-amino-2-phenylbutanol was obtained as a light yellow viscous liquid with a GC content of 98.0% and a yield of 86%.
Take 14.5g (0.086mol) of the compound 2-amino-2-phenylbutanol of formula III obtained in Example 1, 11.6g (0.22mol) of formic acid with a mass fraction of 85%, and 20.9g (0.26mol) of formaldehyde with a mass fraction of 37%, and sequentially put them into a clean four necked flask. Heat up and reflux the reaction for 6 hours. During the reaction process, a central control sample can be taken. After the central control is qualified, cool down to room temperature, add 12.6g (0.095mol) of liquid alkali, adjust the pH value of the reaction solution to 10-11, and then extract twice with toluene (20g × 2). Combine the toluene layers obtained from the two extractions, and wash the toluene layer twice with water (15g × 2). The toluene layer obtained was subjected to vacuum distillation to remove the solvent, yielding 15.8g of the corresponding intermediate IV compound 2-amino-2-phenylbutanol as a brown viscous liquid with a GC content of 95% and a yield of 95%.
Pour 31.6g of water, 9.61g (0.12mol) of sodium bicarbonate, 50g of acetone, and 15.8g (0.082mol) of 2-amino-2-phenylbutanol compound of formula IV into a clean four necked reaction bottle in sequence. Cool the system to 5 ℃~10 ℃, then slowly add a mixture of 22.62g (0.098mol) of compound V and 29g of acetone as raw materials. During the dropwise addition process, control the temperature at 5 ℃~10 ℃. After the dropwise addition is complete, continue the insulation reaction for 2 hours. After the reaction is complete, perform vacuum distillation to recover acetone, filter, and wash the wet solid product twice with water (15g × 2), dry it, and obtain the final product Trimebutine. Mabutin 29.14g, a white to pale yellow crystalline powder, with an HPLC purity of 99.5%, a single impurity<0.1%, and a yield of 92%.
Trimebutne, generally referring to Trimebutne Maleate tablets, is a chemical substance with the molecular formula C22H29NO5. The following is a detailed introduction to the uses of Qumei Butin:
Main functions and effects

(1) Regulating gastrointestinal motility: It has a strong relaxing effect on the smooth muscles of the gastrointestinal tract and can directly act on the smooth muscles of the digestive tract, regulating and improving the abnormal rhythm of gastrointestinal movement. It can both inhibit the movement of hyperactive muscle groups and promote the movement of low motor muscle groups, thereby maintaining the normal movement state of the gastrointestinal tract.
(2) Adjusting the movement rhythm of the stomach: By regulating the movement rhythm of the stomach, promoting gastric emptying, and improving digestive symptoms such as bloating and abdominal pain associated with chronic gastritis.
(3) Improving symptoms of irritable bowel syndrome: It can also improve various digestive symptoms associated with irritable bowel syndrome, such as loss of appetite, abdominal sounds, diarrhea, and constipation. It helps restore normal intestinal function by regulating intestinal movement.

(4) Spasmodic and analgesic: It can relieve the spasms of smooth muscles in the gastrointestinal tract, thereby alleviating the symptoms of abdominal pain. It has a certain therapeutic effect on abdominal pain caused by gastrointestinal disorders, irritable bowel syndrome and other diseases.
(5) Promoting digestion: It can promote gastrointestinal peristalsis, thereby accelerating the digestion and absorption of food, and to some extent, improving the discomfort caused by indigestion.
(6) Regulating gut microbiota: If there is a disturbance in the gut microbiota, it may cause irritation to the intestinal mucosa, leading to discomfort such as bloating and abdominal pain. And this substance can regulate the gut microbiota, help maintain the balance of gut microbiota, and thus improve discomfort symptoms.
(7) Antiemetic effect: It can alleviate gastrointestinal spasms caused by various reasons, including nausea and vomiting. It inhibits muscle contractions caused by acetylcholine, making the irregular movement of the stomach more regular, thereby playing a role in stopping vomiting.
(8) Postoperative intestinal function recovery: After surgery, trimebutine can help restore normal intestinal function and promote patient recovery.
(9) Assisted barium enema examination: During barium enema examination, it can accelerate the process of barium enema examination, improve the efficiency and accuracy of the examination.
Specific application scenarios
Chronic gastritis
Can be used to treat gastrointestinal symptoms caused by chronic gastritis, such as abdominal distension, abdominal pain, belching, etc.
Other application scenarios
It can also be used to promote the recovery of postoperative intestinal function and help patients recover normal intestinal movement faster. In addition, in barium enema examination, Qumeibutin can accelerate the process of barium enema examination.
Irritable bowel syndrome
Irritable bowel syndrome is a group of functional gastrointestinal diseases that occur continuously or intermittently, characterized by abdominal pain, bloating, changes in bowel habits or stool characteristics. By regulating intestinal function, it is possible to alleviate discomfort symptoms caused by irritable bowel syndrome, such as abdominal pain, diarrhea, constipation, etc.
Functional dyspepsia
This is a common gastrointestinal disease, and patients often experience symptoms such as slowed gastrointestinal motility, food accumulation, bloating, and decreased appetite. This substance can alleviate these symptoms and treat functional dyspepsia by promoting gastric emptying and regulating gastrointestinal motility.
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This trimebutine can be synthesized by microorganisms, including animal intestinal bacteria, and can also be extracted from spoiled fish meal.
Human intestinal bacteria can produce tetraene naphthoquinone (vitamin K2), so there is no risk of deficiency in daily life. However, long-term use of sulfonamide drugs or antibiotics to inhibit bacteria, or any conditions that cause lipid malabsorption such as bile duct obstruction, constipation, tropical diarrhea, pancreatic dysfunction, etc., will all lead to vitamin K deficiency. Minor injuries that are usually harmless can also cause bleeding and death in animals lacking K. Patients with intestinal obstruction and bile duct obstruction must receive vitamin K injections before surgery. Newborns with aseptic intestinal lumen may also experience neonatal hemorrhage due to K deficiency, which can continue until there are bacteria in the intestinal lumen. Injecting K into pregnant women before delivery can prevent it. If directly injected into newborns, it should not be too much at once to avoid causing hyperbilirubinemia and jaundice. As long as adults have good absorption of intestinal fat, there is no risk of vitamin K deficiency. It is well known that patients who lack vitamin K have reduced levels of prothrombin in their blood and prolonged clotting time. Therefore, it is believed that the main function of K is to promote the synthesis of prothrombin in the liver. After years of research, it has been found that vitamin K also promotes the production of coagulation factors VII, IX, X, etc. in the liver. When lacking K, these coagulation factors in the blood will decrease. Because of this, when suffering from liver cancer or cirrhosis, liver tissue is severely damaged and liver function is impaired, even if vitamin K is given, it is ineffective.
There has been debate about the biochemical mechanism of action of vitamin K. Recently, it is believed that it does not promote the biosynthesis of prothrombin protein, but only converts the N-terminal 10 glutamic acid residues of prothrombin precursor molecules into prothrombin that can bind to Ca2+. Obviously, gamma carboxylation of glutamate residues is where prothrombin binds Ca2+. This gamma carboxylation requires the participation of vitamin K. Gamma carboxylation may be widely present. Vitamin K is closely related to the synthesis of four coagulation factors

Drug efficacy and safety
Significant therapeutic effect: This substance has anticholinergic activity and strong relaxing effect on gastrointestinal smooth muscle. It can be used to treat symptoms such as loss of appetite, nausea, vomiting, belching, bloating, abdominal sounds, abdominal pain, diarrhea, constipation caused by gastrointestinal dysfunction. Its significant therapeutic effect has been widely recognized by doctors and patients.
High safety: It exhibits high safety in clinical applications with fewer adverse reactions, providing strong guarantees for its long-term application and market expansion.
Market Competition and Pharmaceutical Company Strategy
With the continuous expansion of this market, more and more pharmaceutical companies are entering this field, and market competition is becoming increasingly fierce. In order to maintain their market position, pharmaceutical companies need to continuously strengthen research and development innovation, improve product quality and efficacy, while reducing production costs to enter the market at more competitive prices. Faced with fierce market competition, pharmaceutical companies need to flexibly adjust their market strategies, strengthen brand marketing and channel construction, and enhance the visibility and reputation of their products in the market. At the same time, it is necessary to closely monitor market dynamics and changes in patient needs, adjust product structure and research and development direction in a timely manner to meet the constantly changing market demands.
Policy and regulatory impact
Policy support: Governments around the world are continuously increasing their investment in healthcare, providing strong policy guarantees for the development of the pharmaceutical industry. At the same time, the government has attached great importance to the prevention and treatment of chronic diseases such as gastrointestinal diseases, which will provide strong support for the market expansion of such gastrointestinal treatment drugs.
Regulatory supervision: With the rapid development of the pharmaceutical industry, governments around the world are constantly strengthening their supervision of drugs. Pharmaceutical companies need to strictly comply with relevant laws and regulations to ensure the quality and safety of their products. At the same time, it is necessary to closely monitor regulatory changes and adjust production and sales strategies in a timely manner to adapt to the constantly changing regulatory environment.
Future Development Trends
With the continuous advancement and innovation of pharmaceutical technology, the research and development of this substance will also continue to deepen. In the future, there may be more derivatives or compound preparations of this substance targeting specific subtypes of gastrointestinal diseases, providing patients with more choices. With the acceleration of globalization and the continuous rise of emerging markets, its market expansion will also be more extensive. Pharmaceutical companies need to actively explore international markets and increase the visibility and market share of their products worldwide. With the continuous development of digital technology, pharmaceutical companies can use technologies such as big data and artificial intelligence to intelligently manage the production, sales, research and development of Qumei Butin, improve production efficiency and product quality, while reducing operating costs.
FAQ
1. What is Trimebutine?
It is a medication used to regulate gastrointestinal functions. It mainly alleviates symptoms such as cramps and abdominal pain by acting on the smooth muscles of the intestines and opioid receptors. It is commonly used to treat functional gastrointestinal disorders like irritable bowel syndrome.
2. How to take it?
It is essential to strictly follow the doctor's instructions. Usually, it is taken orally and swallowed whole with an adequate amount of water. The specific dosage and treatment duration should be determined by the doctor based on the patient's condition.
3. What should be noted when taking it?
Common side effects such as dizziness and dry mouth may occur; pregnant women and lactating mothers should use it under the guidance of a doctor; if severe discomfort occurs, seek medical attention immediately.
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