Nicewonger Robb, Fowke April, Nguyen Kathy, Ditto Lori, Caserta Justin, Harris Michele, Baldino Carmen M
ArQule, Inc., 19 Presidential Way, Woburn, MA 01801, USA.
Mol Divers. 2003;7(2-4):247-52. doi: 10.1023/b:modi.0000006907.21070.11.
A microwave-assisted method is described for monoacylating 7-amino-5-aryl-6-cyanopyrido[2,3-d]pyrimidines using excess acid chlorides in pyridine. A diacylated intermediate is effectively deacylated to the product amide by a macroporous-Tris resin. A small library of 17 amides was prepared to validate the method. The integration of commercial microwave technology into the ArQule chemistry platform is also discussed.