ChemInform Abstract: Synthesis and in vitro EGFR (ErbB1) Tyrosine Kinase Inhibitory Activity of 4‐N‐Substituted 6‐Aryl‐7H‐pyrrolo[2,3‐d]pyrimidine‐4‐amines.

Abstract

Synthesis and in vitro EGFR (ErbB1) Tyrosine Kinase Inhibitory Activity of 4-N-Substituted 6-Aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines.-Title compounds like (VIII) are synthesized and tested for their in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity. Both palladium catalyzed and thermal coupling are applied for aromatic substitution with benzylic amines (VII). The two methods result in similar yields, but the Pd coupling has the benefit of lower chemical consumption and reduced reaction times. The SAR is discussed briefly. -(KASPERSEN, S. J.; SOERUM, C.; WILLASSEN, V.; FUGLSETH, E.; KJOEBLI, E.; BJOERKOEY, G.; SUNDBY, E.; HOFF*, B. H.; Eur. J. Med. Chem. 46 (2011) 12, 6002-6014, http://dx.