Synthesis of N-Alkenylated Heterocycles via T3P-Promoted Condensation with Ketones

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Abstract
Herein, we describe a convenient protocol for the synthesis of N-alkenylated heterocycles using abundant ketone electrophiles and T3P as a water scavenger under microwave irradiation. The method can be applied to a diverse range of NH-heterocycles and ketones with good to excellent yields (up to 94%). This procedure is particularly attractive, as it is metal- and base-free, tolerates a variety of functional groups, and offers ease of product purification. The utility of the protocol was exemplified by synthesizing pharmaceutically relevant scaffolds containing the N-alkenyl motif and was further extended to a one-pot reductive amination sequence.
Funding Information
  • Vetenskapsr?det (2018- 05133, 2022-04831)
  • Uppsala Universitet

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