BENZOXAZINO OR BENZOTHIAZINORIFAMYCIN DERIVATIVE

摘要

NEW MATERIAL:The compound of formula I (n is 1-5; X is O or S; R<1> and R<2> are H, 1-4C alkyl or 1-4C hydroxyalkyl) and its salt. USE:A medicine. An antibacterial agent. It is a solid having dark red color, soluble in a number of organic solvents, exhibiting strong antibacterial activity against Gram-positive bacteria and acid-fast bacteria and having low toxicity. It can be used as a production raw material for novel rifamycin derivative of formula II having strong antibacterial activity. It is administered at a rate of 10mg-10g of the active component daily for adult. PREPARATION:The compound of formula I can be produced by reacting a rifamycin derivative of formula III with an amine of formula IV in an organic solvent such as methanol in the presence of a reducing agent such as sodium cyanoborohydride at room temperature for 30min - about 1 month, thereby effecting reductive amination reaction.