Mild and Efficient DBU-Catalyzed Amidation of Cyanoacetates
- 2 April 2009
- journal article
- Published by American Chemical Society (ACS) in Organic Letters
- Vol. 11 (9), 2003-2006
- https://doi.org/10.1021/ol900435t
Abstract
A mild, high-yielding, and practical protocol for the direct amidation of alkyl cyanoacetates using DBU is presented. This method eliminates the need for activation of cyanoacetic acid and/or high temperatures. It has been applied to the large-scale synthesis of CP-690,550-10 (1), a compound under development for the treatment of autoimmune diseases.Keywords
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