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Kilogram synthesis of (R)-(-)-denopamine by Ir/f-amphox catalyzed asymmetric hydrogenation
oleh: Yongpeng Zheng, Xumu Zhang, Runtong Zhang, Baode Ma
Format: | Article |
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Diterbitkan: | KeAi Communications Co. Ltd. 2021-11-01 |
Deskripsi
A practical and efficient two-step synthetic process for the preparation of (R)-(-)-denopamine has been developed. The key step asymmetric hydrogenation was conducted at mild temperature (60 °C) under a hydrogen pressure of 50 atm by using Ir/f-amphox as catalyst at low catalyst loading (S/C = 20 000). Under the optimized condition, the desired product (R)-(-)-denopamine was obtained with 70% total yield and > 99.9% ee after crystallization. The pilot-scale experiment has been performed at 500 g level, showing great potential for the production of high quality active pharmaceutical ingredient (API).