| 摘要 |
<p>4',4'''-Dideoxy-paromomycin, useful as an antibacterial agent, active against gram-positive, gram-negative bacteria and against protozoa is claimed, both per se and in pharmaceutical compositions. The process for its preparation, also claimed, comprises reacting a 6,3',2'',5'',3''',4'''-hexa-O-acyl or benzoyl-6'-O-benzoyl-penta-N- benzyloxycarbonyl-paromomycin with a large excess of carbon disulphide and a strong base, followed by treatment of the reaction mixture with methyl iodide. The resultant 4',4'''- bis-(methylthio thiocarbonate) is reduced with tributyltin hydride, and the hydroxy-protecting groups and amino-protecting groups are successively removed by treatment with methanolic sodium methoxide and by transfer catalytic hydrogenolysis respectively.</p> |
