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- Title
Amination of 5-Spiro-Substituted 3-Hydroxy-1,5-dihydro-2 H -pyrrol-2-ones.
- Authors
Khramtsova, Ekaterina E.; Lystsova, Ekaterina A.; Khokhlova, Evgeniya V.; Dmitriev, Maksim V.; Maslivets, Andrey N.
- Abstract
The 3-hydroxy-1,5-dihydro-2H-pyrrol-2-one motif is a valuable scaffold in drug discovery. The replacement of the 3-oxy fragment in 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones-based compounds with a 3-amino one (3-amino analogs of 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones, 3-amino-1,5-dihydro-2H-pyrrol-2-ones) can play a crucial role in their biological effect. Thus, approaches to 3-amino-1,5-dihydro-2H-pyrrol-2-ones are of significant interest. We developed an approach to 5-spiro-substituted 3-amino-1,5-dihydro-2H-pyrrol-2-ones that could not be obtained using previously reported approaches (reactions of 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones with amines). The developed approach is based on the thermal decomposition of 1,3-disubstituted urea derivatives of 5-spiro-substituted 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones, which were prepared via their reaction with carbodiimides.
- Subjects
CARBODIIMIDES; AMINES; AMINATION
- Publication
Molecules, 2021, Vol 26, Issue 23, p7179
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules26237179