Paul Scherrer Institute, Laboratory for Catalysis and Sustainable Chemistry, Forschungsstrasse 111, CH-5232 Villigen PSI, Switzerland.
F. Hoffmann-La Roche Ltd., Department of Process Chemistry & Catalysis, Grenzacherstrasse 124, CH-4070 Basel, Switzerland, Email:
Chimia (Aarau). 2021 Nov 24;75(11):972-978. doi: 10.2533/chimia.2021.972.
The synthesis of drug substances (DS) requires the continuous effort of the pharma industry to ensure high sustainability standards. The Suzuki-Miyaura cross coupling is a fundamental C-C bond-forming reaction to produce complex DS intermediates. The present contribution points out the way in which the synthesis of DS intermediates by C-C cross coupling can be economically competitive, while minimizing waste by selecting the appropriate heterogeneous catalyst. By comparing homogeneous, immobilized heterogeneous catalysts on silica and metal-organic framework (MOF) catalysts, while considering the perspectives of academia and industry, the critical parameters for a successful industrial application of heterogeneous catalytic Suzuki-Miyaura cross coupling reactions were identified. Heterogeneous catalysts, such as MOFs, may provide a complementary platform for reducing waste and the costs of production related to such transformations.
药物物质(DS)的合成需要制药行业不断努力,以确保高标准的可持续性。铃木-宫浦交叉偶联是生成复杂 DS 中间体的基本 C-C 键形成反应。本研究指出,通过 C-C 交叉偶联合成 DS 中间体可以通过选择合适的多相催化剂在经济上具有竞争力,同时通过最小化废物来实现。通过比较均相、固定在二氧化硅上的多相催化剂和金属有机骨架(MOF)催化剂,并考虑学术界和工业界的观点,确定了用于成功应用多相催化铃木-宫浦交叉偶联反应的关键参数。多相催化剂,如 MOF,可能为减少废物和与这些转化相关的生产成本提供一个互补的平台。