当前位置: X-MOL 学术Green Synth. Catal. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Kilogram synthesis of (R)-(-)-denopamine by Ir/f-amphox catalyzed asymmetric hydrogenation
Green Synthesis and Catalysis ( IF 8.2 ) Pub Date : 2021-11-1 , DOI: 10.1016/j.gresc.2021.09.002
Yongpeng Zheng , Xumu Zhang , Runtong Zhang , Baode Ma

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:

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。
更新日期:2022-01-13
down
wechat
bug