Enantioselective Construction of Multi-Nitrogen-Containing Spirocycles: Asymmetric [3+2] Annulation of 4-Isothiocyanato-pyrazolones with Azodicarboxylates

The 4-isothiocyanatopyrazolones were exploited as a class of efficient synthons for the construction of triazoline derivatives via asymmetric [3+2] annulation with azodicarboxylates, providing a wide range of structurally diverse multi-nitrogen-containing spirocycles in excellent yields (up to 97%) with excellent enantioselectivities (up to 97% ee).

Automated summary

The 4-isothiocyanatopyrazolones are utilized as efficient synthons for the construction of triazoline derivatives through asymmetric [3+2] annulation with azodicarboxylates, yielding a wide range of structurally diverse multi-nitrogen-containing spirocycles in excellent yields (up to 97%) with excellent enantioselectivities (up to 97% ee).