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.
引用
收藏
页码:4930 / 4940
页数:11
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