发明名称 |
Methods for synthesizing substituted tetracycline compounds |
摘要 |
Methods for synthesizing a carboxaldehyde substituted tetracycline compound comprising reacting a tetracycline reactive intermediate under appropriate conditions with carbon monoxide, a palladium catalyst, a phosphine ligand, a silane and a base, such that said carboxaldehyde substituted tetracycline compound is synthesized. The palladium catalyst is chosen from PdCl2 (tBu2PhP)2 dichlorobis (di-tert-butylphenylphosphine palladium (II)] or PdCl2 (DPEPhos) [bis (diphenylphosphinophenyl) ether palladium (II) chloride]. The tetracycline reactive intermediate contains moieties selected from halogens and triflates. Methods of synthesizing a substituted tetracycline compound comprising reacting the carboxaldehyde substituted tetracycline compound under palladium catalyzed coupling conditions, hydrogenolysis conditions or reductive amination conditions. |
申请公布号 |
AU2008275701(B2) |
申请公布日期 |
2013.04.04 |
申请号 |
AU20080275701 |
申请日期 |
2008.07.07 |
申请人 |
PARATEK PHARMACEUTICALS, INC. |
发明人 |
SEYEDI, FARZANEH;GRIER, MARK;WARCHOL, TADEUSZ |
分类号 |
C07C237/26 |
主分类号 |
C07C237/26 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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