2,6-PIPERAZINEDIONE, 4,4'-(1-METHYL-1,2-ETHANEDIYL)BIS-

White or almost white or light beige crystal or crystalline powder, odorless, slightly bitter taste. Soluble in hot water, insoluble in water or ethanol. Melting point 233-234℃(decomposition), melting point 237-239℃. (+)-configuration (Dexrazoxane): [24584-09-6]. Crystallized from aqueous methanol-ether, melting point 193 °C. [α]D+11.35° (C=5, dimethylformamide). Solubility (mg/ml): 10-12 (water), 35-43 (0.1 mol/L hydrochloric acid), 25-34 (0.1 mol/L sodium hydroxide), 6.7-10 (10% ethanol), 1 (methanol), 7.1-10 [water-dimethylformamide (1:1)], 9.7-14.5 [0.1 mol/L citrate buffer (Ph 4) ], 8.7 to 13 [0.1 mol/L boric acid buffer (Ph 9)].

ChEBI: Razoxane is a N-alkylpiperazine.

Suspected carcinogen with experimental carcinogenic and tumorigenic data. Moderately toxic by intraperitoneal route. Experimental teratogenic and reproductive effects. Human systemic effects by ingestion: nausea, thrombocytopenia, leukopenia. Mutation data reported. When heated to decomposition it emits toxic fumes of NOx.

100g of 1, 2-propanediaminetetraacetic acid and 400ml of formamide, under the protection of nitrogen, are heated at 100～110℃ for 1h, and then at 150-155℃ for 4h. The resulting brown solution was evaporated under reduced pressure at 80-90°C to remove the solvent. The residue was dissolved in 120ml methanol and placed in the refrigerator overnight. It was filtered, washed with methanol, and dried in vacuum at 65°C to obtain 62 g of pale beige Razosan fine crystals with a yield of 70% and a melting point of 237-239°C.

Racemate is an antitumor drug. It is used to assist surgical treatment to prevent cancer metastasis, acute leukemia, acute sarcoidosis, and can also be used for lung cancer, gastric cancer, liver cancer, breast cancer, and lymphosarcoma. (+)-configuration is used for cardioprotectant. It is used to protect breast cancer patients and prevent side effects on the heart when chemotherapy with anthracycline antibiotics such as doxorubicin.

Razoxane is an inhibitor of Topo II.