| 摘要 |
PURPOSE:To prepare the titled compound useful as a remedy for tuberculosis, in high yield and purity, by reacting rifamycin S with an oxacyclohexane derivative in the presence of an organic acid, and reacting the product with 1-amino- 4-methyl-piperazine. CONSTITUTION:Rifamycin S is made to react with 1,3-di-alkyl-1,3-diaza-5-oxacyclohexane of formula (R is alkyl) in a solvent such as dimethylformamide in the presence of an organic acid such as acetic acid, oxalic acid, etc., and the reaction product is made to react with 1-amino-4-methylpiperazine at 50-55 deg.C to obtain the objective compound. In the above process, the production of by-products can be suppressed, the rate of reaction is improved and the yield is increased by keeping the pH of the reaction liquid at 5.5-6.8. |
