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Process development and manufacture of potassium 2-fluoro-6-hydroxyphenyltrifluoroborate |
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| Authors: | Lokesh Pawar Ramesh Jayaramaiah Baburaj Krishnan Athimoolam Arunachalampillai Ying Chen Andrew T. Parsons Jo Anna Robinson Jason S. Tedrow |
| Affiliation: | 1. Syngene International Ltd. Biocon Park, Plot 2 & 3, Jigani Link Road, Bangalore, 560099, India;2. Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States |
| Abstract: | The development of a phase-appropriate manufacturing-scale synthesis of potassium 2-fluoro-6-hydroxyphenyltrifluoroborate was achieved. Investigations into improving the yield and robustness indicated that pH of the reaction medium is a critical process parameter. Additional development resulted in replacing tartaric acid with citric acid, resulting in improved process robustness and enabling scale-up to >10 kg. |
| Keywords: | Corresponding author. Trifluoroborate Boronic acid Boron Suzuki coupling |
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