This research demonstrates an efficient reaction to synthesize pyrazoloquinoline derivatives, indicating potential applications.
Herein, we describe a base‐promoted successive (3 + 2) annulation/aromatization reaction of hex‐5‐en‐2‐ynoates with (iso)quinolin‐2‐ium‐2‐yl(tosyl)amides, in which hex‐5‐en‐2‐ynoates act as a novel and regioselectively distinct C2 synthon in this process. The use of β‐ and γ ‐carbons of the substrates for CC bond formation is distinct from the substrate‐controlled divergent reactivity reported previously. The reaction provides an efficient route to highly functionalized pyrazolo[5,1‐a](iso)quinolines, delivering moderate to good yields with exclusive regioselectivity under mild conditions. The products can be further functionalized through reduction or hydrogenation, indicating their potential applications.
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Zhang et al. (2026) studied this question.
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