Keywords

• 3-(2-Chloroethyl)-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
• Paliperidone Impurity
• 41078-70-0

Quick Details

• ProName: Paliperidone Impurity;41078-70-0
• CasNo: 41078-70-0
• Molecular Formula: C11H11ClN2O
• Appearance: White to off white powder
• Application: for drug impurity for drug standards,f...
• DeliveryTime: 1-2 weeks
• PackAge: 10mg/25mg/50mg/100mg/1000mg/5000mg
• Port: Shenzhen/hongkong
• ProductionCapacity: 5000 Metric Ton/Day
• Purity: 95%+ or 98%+
• Storage: -20℃
• LimitNum: 25 Milligram
• Moisture Content: 0.1%
• Impurity: 0.1%

Superiority

Our products are mainly drug impurity reference products, drug standards, analytical chemistry, standard substances, organic chemical synthesis, chemical custom synthesis. For impurity localization, quantification, and quality control in drug development processes. Our laboratory area is more than 5000 square meters, we have more than 20 analytical instruments such as HPLC and MS/LC-MS/GC-MS, we also have TGA, IR and other testing instruments. We have the most advanced SFC preparation separation equipment. We can provide a full range of impurity reference/standard products required for drug development. Most of the impurities are synthesized through the process, there are also many items of impurities can not be obtained by synthetic means, need to be obtained through raw materials, intermediates, crude products or side reactions contained in the trace target compounds, Hubei Moke has a professional impurity preparation and separation technology team, equipped with professional SFC preparation and separation equipment. It can carry out efficient and accurate separation of impurities for complex projects, and solve the problem of impurity preparation for customers.
 

1. We integrate R&D, production and sales. A 5,000-square-meter high-standard bio-intelligent manufacturing base can ensure high quality and fast delivery of products. The professional sales team ensures that you don't need to worry about pre-sales and after-sales.

2. We focus on pharmaceutical standards, pharmaceutical intermediates, pharmaceutical impurity controls, peptide customization, our own laboratory, and undertake customized synthesis projects.

3. We offer products from gram grade to g grade, in addition, some product specifications and packaging can be customized.

4. We have been deeply engaged in the pharmaceutical field for ten years and have rich experience. At present, customers are all over the world, and have been highly recognized and trusted by customers.

5. We can provide a variety of safe ways to transport goods for you to choose.

Details

Paliperidone Impurity

Product Information

• Product Code：P008080

• English Name：Paliperidone Impurity 80

• English Alias：3-(2-chloroethyl)-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one

• CAS No.：41078-70-0

• Molecular Formula：CHClNO

• Molecular Weight：222.67

Advantages

• High-Purity Reference Standard：Confirmed by HPLC (≥99.0%), NMR (1H, 13C), HRMS, and elemental analysis, suitable for Paliperidone impurity analysis and quality control.

• Stability Assurance：Stable for 36 months at -20℃ under light-protected, sealed storage; degradation rate <0.1% in acetonitrile-water solution within 6 months.

Applications

• Quality Control Testing：Used for UPLC-MS/MS detection of Impurity 80 in Paliperidone API and formulations, controlling content to meet ICH Q3A standards (single impurity limit ≤0.1%).

• Process Optimization Research：Monitors Impurity 80 formation during Paliperidone synthesis, reducing generation by >50% by adjusting cyclization temperature (e.g., 60-70℃) and reaction time.

• Method Validation：Serves as a standard for developing impurity detection methods, verifying UPLC resolution (≥3.0) and LOD (0.005 ng/mL).

Background Description

Paliperidone, an atypical antipsychotic, is used for treating schizophrenia. Impurity 80, as a process-related impurity of Paliperidone, may originate from chloroethylation side reactions of the pyridopyrimidine ring or incomplete cyclization during synthesis. Its chloroethyl and pyridopyrimidinone groups may affect drug stability and efficacy. With stricter FDA and EMA requirements for antipsychotic drug impurities, studying Impurity 80 is crucial for ensuring drug quality.

Research Status

• Detection Technology：UPLC-MS/MS with C18 column (1.7μm) and 0.1% formic acid-acetonitrile gradient elution achieves separation within 3 minutes, with LOD of 0.002 ng/mL for trace impurity analysis.

• Formation Mechanism：Formed by reaction of 2-methylpyridopyrimidinone with 2-chloroethyl chloride under alkaline conditions (e.g., sodium carbonate catalysis); optimizing the reaction solvent system (e.g., using DMF instead of ethanol) inhibits side reactions.

• Safety Evaluation：In vitro cytotoxicity shows IC of 156.7 μM against SH-SY5Y cells (Paliperidone IC=8.2 μM), with lower toxicity than the main drug but requiring strict content control. Long-term stability testing is ongoing to monitor degradation under different humidity, light, and temperature conditions.