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