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• W1979941887 abstract "Small molecule TRPV1 antagonists have been a recent focus in the search for pain treatment agents. We herein describe a practical and scalable synthesis of AMG 628 (1), a bis-substituted pyrimidine derivative that was identified as a highly efficacious agent, suitable for clinical development. 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." @default.
• W1979941887 created "2016-06-24" @default.
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• W1979941887 date "2008-03-20" @default.
• W1979941887 modified "2023-09-23" @default.
• W1979941887 title "Practical Synthesis of a Vanilloid Receptor-1 Antagonist" @default.
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• W1979941887 doi "https://doi.org/10.1021/jo8002216" @default.
• W1979941887 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/18351744" @default.
• W1979941887 hasPublicationYear "2008" @default.
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