摘要 |
NEW MATERIAL:The compound of formula I (R<1> and R<2> are H or lower alkyl; R<3> is H, lower alkyl or lower alkoxycarbonyl; R<4> and R<5> are H, lower alkyl, lower alkoxy or halogen) and its salt. EXAMPLE:4-Cyano-3, 8-dimethyl-1,2,3,4,5,6-hexahydro-1, 5-methylimino-9-methoxy- 3-benzoazocine-7,10-dione. USE:Antineoplastic agent. Dose: 50-5,000mg daily. PREPARATION:The compound of formula I can be produced by oxidizing the compound of formula II (R<6> and R<7> are lower alkyl or aralkyl) with e.g. cerium ammonium nitrate, nitric acid, etc. preferably in a 6-16N nitric acid solution, and cyanizing the product with KCN, etc. |