| 摘要 |
<p>NEW MATERIAL:A 5-oxo-3,4,5,6,7,8-hexahydrocarbostyril derivative of formula I (R<1>,<2> are lower alkyl, or R<1> and R<2> together may form an N-containing saturated heterocyclic ring with adjacent N atom). EXAMPLE:6-(Piperidinothiocarbonylthiomethyl)-5-oxo-3, 4, 5, 6, 7, 8-hexahydrocarbostyril. USE:Antibacterial agent especially effective to Mycoplasma. PROCESS:5-Oxo-3,4,5,6,7,8-hexahydrocarbostyril of formula II is reacted with formaldehyde and an amine of formula III in a solvent in the presence of a catalyst at 25- 150 deg.C to afford 6-substituted aminomethyl-5-oxo-3,4,5,6,7,8-hexahydrocarbostyril derivative of formula IV, which is converted to the desired compound I by boiling and refluxing with CS2 in a solvent.</p> |
