Synthesis of pyrrolopyrimidine crf-r1 antagonists containng a tricyclic core via an intramolecular heck reaction

摘要

A synthetic route to pharmaceutically imprortant tricyclic pyrrolopyrimidines was developed.The method employs a palladium-mediated heck cyclization as the critical step in the cinstruction of the final six membered ring.The corticotropin-releasing factor (CRF)peptide/receptor system plays an important role in regulating mammalian stress response,in addition to its participation in other significant biological pathways.