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 |
| |
Authors: | Machetti Fabrizio Bucelli Ilaria Indiani Giovanni Kappe C Oliver Guarna Antonio |
| |
Affiliation: | Istituto di chimica dei composti organometallici del CNR c/o Dipartimento di chimica organica Ugo Schiff, Università degli Studi di Firenze, Firenze, Italy. fabrizio.machetti@unifi.it |
| |
Abstract: | 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 degrees C in the absence of solvent, is characterized by its mildness and ease of workup. A library of amides, was synthesized by combination of methyl esters 1-6 with various amines. In addition, the microwave-assisted automated synthesis of the library was compared with the above conventional parallel synthesis. Microwave synthesis significantly decreased the reaction time from hours to minutes. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|