Paliperidone Impurity
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：C₁₁H₁₁ClN₂O
Molecular Weight：222.67
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.
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).
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.
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 IC₅₀ of 156.7 μM against SH-SY5Y cells (Paliperidone IC₅₀=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.
WhatsAPP: +86 17320513646
E-mail: anna@molcoo.com
NOTE！
We can also customize related analogues and modified peptides including HPLC, MS, 1H-NMR, MS, HPLC, IR, UV, COA, MSDS.
This product is intended for laboratory use only!
WhatsAPP: +86 17320513646
E-mail: anna@molcoo.com
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