发明名称 |
CHIRAL PHOSPHINES FOR PALLADIUM-CATALYZED ASYMMETRIC ALPHA-ARYLATION OF ESTER ENOLATES TO PRODUCE TERTIARY STEREOCENTERS IN HIGH ENANTIOSELECTIVITY |
摘要 |
The disclosure provides new and improved methods for the Pd-catalyzed asymmetric α-arylation of ester compounds, which produce the corresponding α-aryl moiety in high enantioselectivity (generally >90% ee). The present methods utilize a palladium catalyst supported by new (R)—H8-BINOL-derived monophosphine ligands. The method is applicable to a wide variety of aryl triflate substrates having variations in both electronic and steric properties. These aryl triflate substrates react with various α-alkyl (Z)- and/or (E)-0-trimethylsilyl ketene acetals in the presence of a Pd catalyst, (R)—H8-BINOL-derived monophosphine ligand, and a mild activator, for example, LiOAC, to provide the asymmetric α-arylation of ester compounds in high ee. |
申请公布号 |
SG11201400085W(A) |
申请公布日期 |
2014.03.28 |
申请号 |
SG11201400085W |
申请日期 |
2012.08.17 |
申请人 |
NANYANG TECHNOLOGICAL UNIVERSITY |
发明人 |
ZHOU, STEVE, JIANRONG;HUANG, ZHIYAN |
分类号 |
C07F9/50;C07C67/30;C07C69/608;C07C69/612;C07C69/73;C07D215/14;C07D333/38;C07F7/08 |
主分类号 |
C07F9/50 |
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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