title: Mild and efficient DBU-catalyzed amidation of cyanoacetates.
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.
authors.affiliation: Chemical Research and Development, Pfizer, Inc., Eastern Point Road, Groton, Connecticut 06340, USA.
authors.forename: Kristin E
authors.initials: KE
authors.lastname: Price
authors.forename: Claude
authors.initials: C
authors.lastname: Larrivée-Aboussafy
authors.forename: Brett M
authors.initials: BM
authors.lastname: Lillie
authors.forename: Robert W
authors.initials: RW
authors.lastname: McLaughlin
authors.forename: Jason
authors.initials: J
authors.lastname: Mustakis
authors.forename: Kevin W
authors.initials: KW
authors.lastname: Hettenbach
authors.forename: Joel M
authors.initials: JM
authors.lastname: Hawkins
authors.forename: Rajappa
authors.initials: R
authors.lastname: Vaidyanathan