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Synthesis and cross coupling of a highly substituted 2-pyridylboronate: application to the large scale synthesis of a mineralocorticoid antagonist
Authors:Charles BoosDaniel M Bowles  Cuiman CaiAgustin Casimiro-Garcia  Xiangyang ChenCatherine A Hulford  Sandra M JenningsE Jason Kiser  David W Piotrowski  Matthew SammonsRobert A Wade
Institution:Pfizer Global Research & Development, Groton/New London Laboratories, Pfizer Inc., Groton, CT 06340, United States
Abstract:The large scale synthesis of functionalized 2-pyridylboronate 8 and optimization of its Suzuki-Miyaura coupling to chloropyrazoline (R)-7 to provide a scalable synthesis of mineralocorticoid antagonist (R)-1 is described.
Keywords:Suzuki-Miyaura coupling  2-Pyridylboronate  Pyrazoline  Large-scale synthesis
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