Development and Scale-Up of the Electrochemical Dehalogenation for the Synthesis of a Key Intermediate for NS5A Inhibitors
Development and Scale-Up of the Electrochemical Dehalogenation for the Synthesis of a Key Intermediate for NS5A Inhibitors
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DOI：
10.1021/acs.oprd.5b00272
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发表时间：
2015-10-01
影响因子：
3.4
通讯作者：
Waldvogel, Siegfried R.
中科院分区：
文献类型：
--
作者：
Guetz, Christoph;Baenziger, Markus;Waldvogel, Siegfried R.
在分批式电解池中，对螺环丙烷-脯氨酸衍生物在含铅青铜上进行了二次电化学脱卤，收率高，选择性好。通过流动电解池进行升级也取得了成功。详细阐述了采用单细胞传代完成转化的条件。这里的关键是阴极的直接冷却和确保良好的层流。
The electrochemical 2-fold dehalogenation of a spirocyclopropane-proline derivative at leaded bronze was scaled-up in a divided batch-type electrolysis cell in good yield and excellent selectivity. The upscaling via a flow electrolysis cell was also successful. Conditions were elaborated employing a single cell passage for complete conversion. The keys here are the direct cooling of the cathode and ensuring a good laminar flow.