Development and Scale-Up of the Electrochemical Dehalogenation for the Synthesis of a Key Intermediate for NS5A Inhibitors

作者：Guetz Christoph; Baenziger Markus; Bucher Christoph; Galvao Tomas R; Waldvogel Siegfried R^*

来源：Organic Process Research & Development, 2015, 19(10): 1428-1433.

DOI：10.1021/acs.oprd.5b00272

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.

• 出版日期2015-10