1144516-17-5
1144516-17-5
CAS: 1144516-17-5
Molecular Formula: C31H27ClN6O5
1144516-17-5 - Names and Identifiers
1144516-17-5 - Physico-chemical Properties
| Molecular Formula | C31H27ClN6O5 |
| Molar Mass | 599.04 |
| Density | 1.44±0.1 g/cm3(Predicted) |
| pKa | 8.39±0.20(Predicted) |
1144516-17-5 - References
| Introduction | Neratinib is a drug developed by Puma Biotechnology company in the United States to treat breast cancer, is a highly selective human epidermal growth factor receptor (EGFR) and HER-2 inhibitors. Clinical studies have shown that the treatment of early HER-2 positive breast cancer, lenatinib is significantly better than Roche Herceptin (Herceptin). The structure and properties of the impurity OPCQ of lenatinib and lenatinib are very similar, and the solubility in common organic solvents is very small, which is difficult to purify and separate. |
| preparation method | lenatinib was stored for 6 months in a 40 °c/75% RH stable chamber and 1 month in a 56 °c oven. Samples were pulled regularly for testing. Samples were dissolved in 50/50 volume/volume acetonitrile/water at a concentration of about 0.5mg/mL. The solution was examined directly using the LC/MS method to identify any degradation products and impurities at six months, the resulting impurities including lenatinib impurity OPCQ. Synthesis of lenatinib impurity OPCQ: addition reaction of lenatinib with dimethylamine. The dimethylamine used in the reaction is 2mol/L tetrahydrofuran solution, and the boiling point of dimethylamine is only 6.9 ℃, which is easy to volatilize. Four times equivalent dimethylamine and lenatinib are used for tube sealing reaction under high pressure, after 12 hours of reaction, 4 times of dimethylamine was added, and the reaction was continued for another 12 hours. The reaction was basically complete, with more by-products, but the target product was bright and far away, after separation and purification, the yield was 30%. |
Last Update：2024-04-09 15:16:58
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