Mild and efficient DBU-catalyzed amidation of cyanoacetates.

Autor: Price KE; Chemical Research and Development, Pfizer, Inc., Eastern Point Road, Groton, Connecticut 06340, USA., Larrivée-Aboussafy C, Lillie BM, McLaughlin RW, Mustakis J, Hettenbach KW, Hawkins JM, Vaidyanathan R
Jazyk: angličtina
Zdroj: Organic letters [Org Lett] 2009 May 07; Vol. 11 (9), pp. 2003-6.
DOI: 10.1021/ol900435t
Abstrakt: 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.
Databáze: MEDLINE