Journal
ORGANIC LETTERS
Volume 11, Issue 9, Pages 2003-2006Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol900435t
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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.
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