Kilogram synthesis of (R)-(-)-denopamine by Ir/f-amphox catalyzed asymmetric hydrogenation
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 = 2...
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| Autores principales: | , , , |
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| Formato: | article |
| Lenguaje: | EN |
| Publicado: |
KeAi Communications Co. Ltd.
2021
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| Materias: | |
| Acceso en línea: | https://doaj.org/article/19ed00e7bde540b28648ba550eba3ae8 |
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| Sumario: | 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). |
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