[摘要]：(Heterocyclic Compounds (More Than One Hetero Atom)) Section Small mol. TRPV1 antagonists have been a recent focus in the search for pain treatment agents. A practical and scalable synthesis of AMG 628 (I), a bis-substituted pyrimidine deriv. that was identified as a highly efficacious agent, suitable for clin. development is reported. Highlights of our approach include a practical route to a substituted benzothiazole, a scalable synthesis of an enantiopure piperazine fragment, and identification of conditions for selective coupling reactions on 2,6-dichloropyrimidine, to access the active pharmaceutical ingredient in high purity and overall yield.
