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One-Pot Reductive Amination and Suzuki-Miyaura Cross-Coupling of Formyl Aryl and Heteroaryl MIDA Boronates in Array Format
被引:31
|作者:
Grob, Jonathan E.
[1
]
Nunez, Jill
[1
]
Dechantsreiter, Michael A.
[1
]
Hamann, Lawrence G.
[1
]
机构:
[1] Novartis Inst BioMed Res Inc, Cambridge, MA 02139 USA
关键词:
BORONIC ACIDS;
BIOLOGICAL EVALUATION;
EFFICIENT;
COMPLEXES;
RECEPTOR;
D O I:
10.1021/jo2005928
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
Formyl-substituted aryl and heteroaryl MIDA boronates were prepared by a DMSO-free method and used in the first reported one-pot reductive amination-Suzuki-Miyaura cross-coupling sequence. This sequence was then carried out in parallel array format, using microwave-assisted in situ release cross-coupling of MLDA boronates to generate a library with diversity along two axes, affording rapid and convenient access to an array of druglike molecules.
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页码:4930 / 4940
页数:11
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