Quetiapine Fumarate Powder CAS 111974-72-2

Quetiapine fumarate powder is a dibenzothiazepine derivative. It exists as a white to off-white crystalline powder that is practically insoluble in water but soluble in glacial acetic acid. The drug has a melting point range of 170-174°C. The odorless and tasteless characteristics make it more convenient to handle and store, while also reducing the risk of confusion with other substances. Keep away from oxidants during storage. When recycling, it is recommended to dissolve and mix in combustible solvents in a chemical incinerator equipped with post combustion and washing devices. It is a new generation of atypical psychotropic drugs. Zeneca was first listed in the UK in November 1997. Clinically used as a first-line medication for the treatment of schizophrenia.

Quetiapine fumarate powder is an atypical antipsychotic drug that exerts therapeutic effects by antagonizing dopamine receptors and 5-hydroxytryptamine receptors. Its use covers a wide range of core psychiatric diseases and extends to adjuvant therapy and special scenario applications. The specific uses are as follows:

Core Indications: Schizophrenia and Bipolar Disorder

 

1. Treatment for schizophrenia
It is a first-line treatment drug for schizophrenia, which has significant therapeutic effects on both positive symptoms (such as hallucinations, delusions, and thinking disorders) and negative symptoms (such as emotional apathy and social withdrawal). Its mechanism of action reduces dopamine overactivity by blocking dopamine D2 receptors, while antagonizing 5-HT2 receptors improves negative symptoms. Clinical trials have shown that its short-term efficacy is comparable to traditional drugs such as chlorpromazine and haloperidol, and long-term use does not cause persistent prolactin elevation, reducing the risk of endocrine disorders.

 

2. Management of bipolar disorder
Manic episode: As an emotional stabilizer, it can quickly control the manic symptoms of bipolar I disorder (such as high mood, impulsive behavior, sleep disorders) by regulating 5-HT2 and D2 receptors to balance emotional fluctuations.
Mixed episode: For patients with both manic and depressive characteristics, its bidirectional regulatory effect can reduce extreme emotional changes and lower the risk of suicide.
Adjuvant therapy: When used in combination with lithium salts or sodium valproate, it can enhance efficacy and shorten the duration of attacks, especially for refractory cases.

Adjuvant therapy: extended to depression and other mental disorders

 

1. Adjuvant treatment for depression
For patients with depression accompanied by psychotic symptoms such as hallucinations and delusions, Ping can enhance the effectiveness of antidepressants, reduce anxiety, suicidal ideation, and sleep disorders. The mechanism may involve partial activation of 5-HT1A receptors, improving mood swings and cognitive function.

2. Anxiety disorders and post-traumatic stress disorder (PTSD)
Anxiety symptoms: By regulating the amygdala prefrontal cortex pathway, excessive alertness and fear responses are reduced, alleviating the core symptoms of generalized anxiety disorder (GAD).

 

PTSD treatment: It has an improvement effect on post-traumatic flashback, avoidance behavior, and high alertness, especially suitable for complex cases with comorbid psychiatric characteristics.
3. Mental disorders due to physical diseases
Quetiapine fumarate is one of the preferred drugs for secondary psychiatric symptoms such as hallucinations, delusions, and agitation in physical diseases such as Parkinson's disease and stroke, due to its low risk of extrapyramidal reactions (EPS).

Special scenario application: Insomnia and elderly patient management

 

1. Treatment of Stubborn Insomnia
Low dose quetiapine fumarate powder (25-100mg/day) can produce sedative effects by antagonizing histamine H1 receptors, shorten sleep onset time, and prolong sleep duration. Its advantage lies in its non addictive nature and minimal impact on sleep structure, making it suitable for patients who are tolerant or dependent on benzodiazepines.

 

2. Management of Elderly Mental Disorders
Dose adjustment: Due to slowed metabolism in elderly individuals, the initial dose should be reduced to 25mg/day and gradually increased to the effective dose (usually 150-300mg/day) to reduce adverse reactions such as hypotension and dizziness.
Comorbidity treatment: For elderly patients with cardiovascular disease and diabetes, quetiapine fumarate does not significantly affect blood lipid and blood sugar levels, and its safety is better than that of traditional antipsychotics.

Add dibenzo [b, f][1, 4] azathio-11-(10h) ketone and toluene to the reaction flask, add sodium carbonate solution, cool down, drop the solution of Triphosgene dissolved in toluene, keep the temperature at 0 ℃ for 1 hour, raise the temperature to 20 ~ 30 ℃ and keep the temperature for 2 hours, inject nitrogen for 5 ~ 10 minutes before the end of the reaction, and the tail gas enters the absorption tank. Separate the water layer, wash the toluene layer twice with dilute hydrochloric acid, and then wash it twice with water. Take the toluene layer and dry it with anhydrous sodium sulfate, filter the desiccant to obtain the toluene solution of chlorinated product, and directly enter the next condensation reaction. 200g (1.15mol) of 1- (2-hydroxyethoxy) ethyl piperazine and solid potassium carbonate were added to the toluene solution containing chlorinated products in the previous step three times. After each feeding, they were heated and refluxed for 8 hours, and the refluxing reaction lasted for 24 hours. After the reaction, it is reduced to room temperature, mixed with water to dissolve the solid, and the water layer is removed. The toluene layer is washed with water twice, dried with anhydrous sodium sulfate, filtered out the desiccant, and evaporated the toluene solvent under reduced pressure to obtain quetiapine oil. Add absolute ethanol to quetiapine oil, stir to dissolve, add fumaric acid, heat and reflux for 1 hour, lower the temperature for crystallization, filter, and dry to obtain quetiapine semifumarate. The content is 99.2% (HPLC), and the overall yield is 81.2%.

• Add isopropanol and water into No. 1 three mouth bottle, add mercaptosalicylic acid and o-chloronitrobenzene under stirring, replace with nitrogen, the system is turbid liquid, and then add the solution and water prepared by sodium hydroxide and water; Refluxing reaction for 10-12h, TLC detection of sulfhydryl salicylic acid, cooling to 20-30 ℃ after reaction, adjusting pH ＜ 1 with concentrated hydrochloric acid, stirring crystallization, filtration, washing with water and toluene respectively for 2 times, and drying under reduced pressure to obtain 2- (2-nitrophenylmercapto) benzoic acid, with a molar yield of 90% and a purity of 98.5%.
• Add 2- (2-nitrophenylmercapto) benzoic acid and dichloromethane into No. 2 three mouth bottle, drop dichlorosulfoxide, conduct heat preservation reaction, spin dry, dilute the oil with dichloromethane, add n-[2- (2-hydroxyethoxy) ethyl] piperazine, triethylamine and dichloromethane into No. 3 three mouth bottle, stir to reduce the temperature, drop the above dichloromethane diluent into the system, react in layers, wash the organic layer with sodium carbonate and water respectively, spin dry to obtain piperazine condensate.
• Heat up the piperazine condensate and formic acid, add iron powder, conduct heat preservation reaction, filter and dry the formic acid after the raw material reaction is detected by TLC, add methylene chloride and water, adjust the pH with sodium bicarbonate solution, separate the layers, extract with methylene chloride for 3 times, combine the organic layers, spin dry to obtain quetiapine, with a molar yield of 92.0% and a purity of 99.8%.
• Quetiapine and fumaric acid were salted in methanol and dried to obtain quetiapine semi fumarate with a molar yield of 92.0% and a purity Quetiapine fumarate powder of 99.5%.

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