Parallel Synthesis of an Amide Library Based on the 6,8-Dioxa-3-azabicyclo[3.2.1]octane Scaffold by Direct Aminolysis of Methyl Esters
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- 作者：Fabrizio Machetti ; Ilaria Bucelli ; Giovanni Indiani ; C. Oliver Kappe ; Antonio Guarna
- 刊名：Journal of Combinatorial Chemistry
- 出版年：2007
- 出版时间：May 2007
- 年：2007
- 卷：9
- 期：3
- 页码：454 - 461
- 全文大小：147K
- 年卷期：v.9,no.3(May 2007)
- ISSN：1520-4774
文摘
An efficient synthesis of unsubstituted and substituted amides based on the 6,8-dioxa-3-azabicyclo[3.2.1]octane scaffold is described. The reaction, carried out at 60 
C in the absence of solvent, is characterizedby its mildness and ease of workup. A library of amides, was synthesized by combination of methyl esters1-6 with various amines. In addition, the microwave-assisted automated synthesis of the library was comparedwith the above conventional parallel synthesis. Microwave synthesis significantly decreased the reactiontime from hours to minutes.
C in the absence of solvent, is characterizedby its mildness and ease of workup. A library of amides, was synthesized by combination of methyl esters1-6 with various amines. In addition, the microwave-assisted automated synthesis of the library was comparedwith the above conventional parallel synthesis. Microwave synthesis significantly decreased the reactiontime from hours to minutes.