Development of a reversible p2y12r antagonist, azd1283-discovery research and large-scale chemistry

This chapter describes the AstraZeneca discovery activities from the identification of a new lead series using high-Throughput screening to the selection of AZD1283 as a P2Y 12 R antagonist for clinical development. This is followed by a discussion of the synthetic development efforts starting with the early procedure used to prepare the first few milligrams in discovery to the development of a multi-kilogram synthesis capable of supporting the market needs of the drug product. © 2018 American Chemical Society.