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= 20000). 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).

中文翻译：

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Ir/f-amphox催化不对称氢化合成千克(R)-(-)-地诺巴胺

已经开发了一种实用且有效的两步合成方法来制备 (R)-(-)-地诺巴胺。关键步骤不对称氢化是在温和的温度（60 ℃）和 50 atm 的氢气压力下，使用 Ir/f-amphox 作为催化剂在低催化剂负载（S/C= 20000）下进行的。在优化条件下，得到所需产物(R)-(-)-地诺巴胺，总收率70%，结晶后ee>99.9%。中试规模实验已在 500 g 水平上进行，显示出生产高质量活性药物成分 (API) 的巨大潜力。