C-N Bond Formation By Consecutive Continuous-Flow Reductions Towards A Medicinally Relevant Piperazine Derivative
MOLECULES(2021)
摘要
A new, continuous-flow consecutive reduction method was developed for the C-N bond formation in the synthesis of the key intermediate of the antipsychotic drug cariprazine. The two-step procedure consists of a DIBAL-H mediated selective ester reduction conducted in a novel, miniature alternating diameter reactor, followed by reductive amination using catalytic hydrogenation on 5% Pt/C. The connection of the optimized modules was accomplished using an at-line extraction to prevent precipitation of the aluminum salt byproducts.
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关键词
flow chemistry, C-N bond formation, consecutive reductions, cariprazine
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