952138-97-5Relevant articles and documents
A concise synthesis of a novel insulin-like growth factor i receptor (IGF-IR) inhibitor
Slade, Joel,Bajwa, Joginder,Liu, Hui,Parker, David,Vivelo, James,Chen, Guang-Pei,Calienni, John,Villhauer, Edwin,Prasad, Kapa,Repic, Oljan,Blacklock, Thomas J.
, p. 825 - 835 (2007)
An efficient synthesis of a potent insulin-like growth factor I receptor (IGF-IR) inhibitor AEW541 (1) is described. The key step in the synthesis is the cis-selective reductive animation of cyclobutanone, which sets up the desired 1,3-stereochemistry of the cyclobutane ring. The amino group thus generated is used as a handle to build the pyrrolopyrimidine ring. The final step resulting in 1 is accomplished by alkylation of in situ generated mesylate with azetidine.