A General Kilogram Scale Protocol for Suzuki–Miyaura Cross-Coupling in Water with TPGS-750-M Surfactant,Organic Process Research & Development

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A General Kilogram Scale Protocol for Suzuki–Miyaura Cross-Coupling in Water with TPGS-750-M Surfactant
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-07-15 , DOI: 10.1021/acs.oprd.0c00281
Michael Parmentier ₁ , Mona Wagner ₁ , Regina Wickendick ₁ , Markus Baenziger ₁ , Audrey Langlois ₁ , Fabrice Gallou ₁

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The development of a kilogram scale protocol for a Suzuki–Miyaura cross-coupling step toward the synthesis of the drug candidate LSZ102 is described. Particularly, the use of the surfactant TPGS-750-M in water as a medium for the transformation and its impact on the selectivity and quality are reported. Minimization of typical impurities generated during the cross-coupling (e.g., dehalogenation) has been in focus during our study. The environmental and cost impacts using such a process are also discussed.

中文翻译：

铃木-宫浦与TPGS-750-M表面活性剂在水中的交叉偶合的通用千克尺度协议

描述了铃木-宫浦交叉偶联步骤朝着候选药物LSZ102的合成的千克规模方案的发展。特别地，报道了表面活性剂TPGS-750-M在水中作为转化介质的用途及其对选择性和质量的影响。在我们的研究中，将最小化交叉偶联过程中产生的典型杂质（例如脱卤）作为重点。还讨论了使用这种方法对环境和成本的影响。

更新日期：2020-08-21

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