摘要 |
<P>PROBLEM TO BE SOLVED: To provide a method for synthesizing a substituted tetracycline compound. <P>SOLUTION: The method for synthesizing the carboxaldehyde-substituted tetracycline compound comprises reacting a tetracycline reactive intermediate under appropriate conditions with carbon monoxide, a palladium catalyst, a phosphine ligand, a silane and a base, so that the carboxaldehyde-substituted tetracycline compound is synthesized. The palladium catalyst is chosen from PdCl<SB>2</SB>(tBu<SB>2</SB>PhP)<SB>2</SB>dichlorobis[di-tert-butylphenylphosphine palladium (II)] or PdCl<SB>2</SB>(DPEPhos)[bis(diphenylphosphinophenyl)ether palladium (II) chloride]. The tetracycline reactive intermediate contains moieties selected from halogens and triflates. <P>COPYRIGHT: (C)2011,JPO&INPIT |