Boiling point: 617.77℃ (rough estimate)
Density: 1.3783 (rough estimate)
Refractive index: 1.6400 (estimate)
Epirubicin is one of the drugs selected to treat solid tumors. It acts directly on DNA, interferes with and prevents DNA replication and transcription. It affects the function of mitochondria by inhibiting the activities of respiratory enzymes such as succinate oxidase and NADPH oxidase. It has been found that it can induce apoptosis of cancer cells, which may occur through the mitochondrial pathway of apoptosis. Due to its excretion through the hepatobiliary system, the patients with liver dysfunction should be reduced to avoid accumulation of poisoning; for patients with moderate liver dysfunction (bilirubin 1.4-3mg / 100ml or BSP retention 9-15%), the dosage should be reduced by 50%; for patients with severe liver dysfunction (bilirubin > 3mg / 100ml or BSP retention > 15%), the dosage should be reduced by 75%; for patients with moderate renal dysfunction, there is no need to reduce the dosage, because Only a small amount of the drug is excreted through the kidney. The usage is intravenous administration. It is suggested to inject normal saline first to check the patency of the infusion tube and after the injection needle is indeed in the vein, then to give medicine through the patency of the infusion tube. This method can reduce the risk of drug spillover and ensure that the vein is flushed with saline after administration. If epirubicin overflows the vein during injection, it will cause serious tissue damage or even necrosis. If the same vein is injected in small vein or repeatedly, it will cause venous sclerosis. It cannot be mixed with heparin, because the chemical properties of the two are not compatible, and precipitation reaction will occur at a certain concentration. It can be used with other anti-tumor drugs, but the dosage of epirubicin should be reduced, not in the same syringe Mixed drugs.
For breast cancer, ovarian cancer, digestive tract cancer (such as advanced gastric cancer, advanced rectal and colon cancer), malignant lymphoma, lung cancer and malignant melanoma, etc.
Compound (I) is N-acylated with trifluoroacetic anhydride to protect the amino group to give compound (II). Reoxidation to ketone (III) followed by reduction to alcohol (IV). Removal of the ether bond under the action of an acid followed by esterification with trifluoroacetic anhydride to compound (VI), followed by selective chlorination, afforded the desired side chain (VII). Compound (VIII) is reacted with dimethylacetal to form ketal (IX), and then reacted with the above-prepared side chain (VII) to hydrolyze the obtained compound (X) to obtain epirubicin.