Catalyst/Solvent Free Decarboxylation of α-Carboxylic Acids Grafted at N2 of 6-Arylpyridazin-3(2H)-ones and 4-Arylphthalazin-1(2H)-ones: Crystallography of N-Alkyl Derivatives and Intermediates
The straightforward decarboxylation of pyridazin-3(2H)-one-2-yl acetic acids and some of its alkyl homologues was achieved without the need for a catalyst and in solvent-free conditions by simple heating above the melting points. By this procedure N-alkylated pyridazin-3(2H)-ones 4a–e, tetrahydrophthalazin-1(2H)-one 5 and phthalazin-1(2H)-one 6 were obtained and the N-alkylated pyridazin-3(2H)-ones 4d,e, tetrahydrophthalazin-1(2H)-one 5 and phthalazin-1(2H)-one 6 were investigated by X-ray diffraction analysis and their supramolecular features were investigated by Hirshfeld analysis and CSD structure investigation, which revealed among other things that the 5,6,7,8-tetrahydrophthalazine framework had not been previously reported. We also investigated the ester precursors 2c,d. The reaction is feasible for a multi-gram scale approach. The compounds show weak hydrogen bonds of type C-H···O and C-H···Cl and in some cases π-stacking interactions. For some of the compounds we observed recurrent C-H···O patterns such as bifurcated H-bonds by switching the C=O acceptor.
Authors
- Sergiu G. Shova (ORCID: https://orcid.org/0000-0002-1222-4373)
- Marcel Mirel Popa (ORCID: https://orcid.org/0000-0002-4161-9972)
- Florea Dumitraşcu (ORCID: https://orcid.org/0000-0002-5743-8519)
- Constantin Drăghici
Institutions
- Institute of Macromolecular Chemistry (UA)
- Romanian Academy (RO)
Publication Details
- Journal
- Crystals
- Published
- 2026-10-19
- DOI
- https://doi.org/10.3390/cryst16100672
- Primary Topic
- Synthesis of heterocyclic compounds
- Type
- article
- Field-Weighted Citation Impact
- 0.00