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Communication | Special issue | Vol 62, No. 1, 2004, pp.191-195
Published online, 14th November, 2003
DOI: 10.3987/COM-03-S(P)41
Synthesis of Pyrrolopyrimidine CRF-R1 Antagonists Containing a Tricyclic Core via an Intramolecular Heck Reaction

Brian Dyck* and James R. McCarthy

*Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 10555 Science Center Drive, San Diego, CA 92121, U.S.A.


A synthetic route to pharmaceutically important tricyclic pyrrolopyrimidines was developed. The method employs a palladium-mediated Heck cyclization as the critical step in the construction of the final six membered ring.