Tofacitinib Impurity 43 NEW

Product Information

• Product Code：T006151

• English Name：Tofacitinib Impurity 151

• English Alias：N,4-dimethylpiperidin-3-amine

• CAS No.：1824188-05-7

• Molecular Formula：C₇H₁₆N₂

• Molecular Weight：128.22

Advantages

• High-Purity Reference Standard：Confirmed by HPLC (≥99.0%), NMR (1H, 13C), and HRMS, suitable for precise analysis of Tofacitinib impurities.

• Stability Assurance：Stable for 24 months at 2-8℃ under light-protected, sealed storage; degradation rate <0.3% in methanol solution within 1 month.

Applications

• Quality Control Testing：Used for HPLC and GC-MS detection of Impurity 151 in Tofacitinib API and formulations, controlling impurity content to meet ICH Q3A standards (≤0.1%).

• Process Optimization Research：Monitors impurity formation during Tofacitinib synthesis, reducing generation by >50% by adjusting alkylation temperature (e.g., 50-60℃) and reaction time.

• Method Validation：Serves as a standard for developing impurity detection methods, verifying HPLC resolution (≥2.0) and LOD (0.01 ng/mL).

Background Description

Research Status

• Detection Technology：GC-MS with DB-5MS column (30m×0.25mm×0.25μm) and temperature programming (80℃ initial, 10℃/min to 250℃) achieves separation within 6 minutes, with LOD of 0.005 ng/mL for trace analysis.

• Formation Mechanism：Formed by reaction of 4-methylpiperidin-3-amine with methylation reagents (e.g., iodomethane) under alkaline conditions (e.g., potassium carbonate catalysis); optimizing base dosage and reaction solvent (e.g., DMF) inhibits side reactions.

• Safety Evaluation：In vitro cytotoxicity shows IC₅₀ of 214.3 μM against Jurkat cells (Tofacitinib IC₅₀=12.7 μM), with low toxicity but requiring ≤0.1% limit. Long-term stability testing is ongoing for degradation.