The utilization of DMF as a dual synthon to serve as a methine source to introduce C2 carbon and nitrogen source to incorporate amino functionality in the 4th position of quinoline under Cu-catalysis.
In this study, we developed a convenient and efficient two‐step method for the synthesis of ynones in a flow reactor, through the generation of lithium acetylide and its subsequent reactions with acid chlorides. Using this approach, we obtained the ynones in moderate to good yields at room temperature. Moreover, we transformed the ynones into pyrazole derivatives through coupling with hydrazines. This transition metal‐free process, mild reaction conditions, and broad functional group tolerance are all attractive features in comparison with conventional bench‐top methods.
A highly efficient and convenient Negishi cross‐coupling reaction has been developed for the synthesis of unsymmetrical alkynes and enynes in a continuous‐flow process. The reaction proceeds through an in situ generated alkynylzinc reagent by the reaction of lithium acetylide with zinc halide at room temperature followed by a cross‐coupling reaction with aryl or vinyl iodides. The notable features of this work compared to the conventional benchtop method are mild reaction conditions, good to excellent yields, broad functional‐group compatibility, short residence time (73 sec) and especially desilylation of TMS group with the residence time of only 10.5 sec.
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