Long-range diastereoselectivity in Ugi reactions of 2-substituted dihydrobenzoxazepines
2011

Good Selectivity in Ugi Reactions of Cyclic Imines

publication Evidence: moderate

Author Information

Author(s): Banfi Luca, Basso Andrea, Cerulli Valentina, Rocca Valeria, Riva Renata

Primary Institution: Department of Chemistry and Industrial Chemistry, University of Genova

Hypothesis

Can 2-substituted dihydrobenzoxazepines exhibit good diastereoselectivity in Ugi reactions despite the distance between stereogenic centers?

Conclusion

The study found that Ugi reactions of 2-substituted dihydrobenzoxazepines can achieve high diastereoselectivity, with ratios up to 9:1.

Supporting Evidence

  • The Ugi reaction of 2-substituted dihydrobenzoxazepines showed diastereoisomeric ratios up to 9:1.
  • This is the first example of 1,4 asymmetric induction in an Ugi reaction.
  • The methodology allows for the diversity-oriented synthesis of various tetrahydrobenzoxazepines.

Takeaway

This research shows that certain chemical reactions can create different versions of a molecule, even when the parts are far apart, which is pretty cool!

Methodology

The study involved synthesizing chiral 7-membered cyclic imines and testing their diastereoselectivity in Ugi reactions.

Limitations

The yields were moderate due to side reactions, and the relative configuration of the major adducts has not been unambiguously proven.

Digital Object Identifier (DOI)

10.3762/bjoc.7.109

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