A Concise Synthesis of a Novel Insulin-Like Growth Factor I Receptor (IGF-IR) Inhibitor†

作者: Joel Slade , Joginder Bajwa , Hui Liu , David Parker , James Vivelo

DOI: 10.1021/OP700052U

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摘要: An efficient synthesis of a potent insulin-like growth factor I receptor (IGF-IR) inhibitor AEW541 (1) is described. The key step in the cis-selective reductive amination cyclobutanone, which sets up desired 1,3-stereochemistry cyclobutane ring. amino group thus generated used as handle to build pyrrolopyrimidine final resulting 1 accomplished by alkylation situ mesylate with azetidine.

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