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Synthesis and cross coupling of a highly substituted 2-pyridylboronate: application to the large scale synthesis of a mineralocorticoid antagonist |
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| 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 |
| Affiliation: | 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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