One-Pot Reductive Amination and Suzuki鈥揗iyaura Cross-Coupling of Formyl Aryl and Heteroaryl MIDA Boronates in Array Format

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• 作者：Jonathan E. Grob ; Jill Nunez ; Michael A. Dechantsreiter ; Lawrence G. Hamann
• 刊名：Journal of Organic Chemistry
• 出版年：2011
• 出版时间：June 17, 2011
• 年：2011
• 卷：76
• 期：12
• 页码：4930-4940
• 全文大小：949K
• 年卷期：v.76,no.12(June 17, 2011)
• ISSN：1520-6904

文摘

Formyl-substituted aryl and heteroaryl MIDA boronates were prepared by a DMSO-free method and used in the first reported one-pot reductive amination鈥揝uzuki鈥揗iyaura cross-coupling sequence. This sequence was then carried out in parallel array format, using microwave-assisted in situ release cross-coupling of MIDA boronates to generate a library with diversity along two axes, affording rapid and convenient access to an array of druglike molecules.