Total Synthesis of (±)-Paroxetine by Diastereoconvergent Cobalt-Catalysed Arylation

نویسندگان

  • Carole F Despiau
  • Andrew P Dominey
  • David C Harrowven
  • Bruno Linclau
چکیده

A total synthesis of paroxetine is reported, with a diastereoselective and diastereoconvergent cobalt-catalysed sp3-sp2 coupling reaction involving a 3-substituted 4-bromo-N-Boc-piperidine (Boc = tert-butoxycarbonyl) substrate as a key step. A 9:1 diastereoselectivity was obtained, while a control experiment involving a conformationally locked 3-substituted 4-bromo-tert-butyl cyclohexane ring proceeded with essentially complete stereoselectivity.

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عنوان ژورنال:

دوره 2014  شماره 

صفحات  -

تاریخ انتشار 2014