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  • Open access
  • 48 Reads
Benzylation of 2-Benzylisoindoline-1,3-diones via Photoinduced Electron Transfer. Photoinitiated Tin-Free Radical Additions to Cyclic Imides
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Photoinduced electron transfer (PET) from arylacetates to 2-benzyl-isoindoline-1,3-diones (N-benzylphthalimides) in aqueous solution furnishes 3-benzylated 2-benzyl-3-hydroxyisoindolin-1-ones in high yields. The procedure constitutes an efficient photoinitiated tin-free radical alternative to the Grignard reaction en route to precursors to phenanthrene lactam alkaloids.
  • Open access
  • 66 Reads
Alpha Fluorination of Ketones by F+ Transfer Using a Precursor of MnF4
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Alpha fluorination of ketones is carried out under very mild conditions by using manganese (IV) dioxide and pyridinium polyhydrogenofluoride. Working up is simple and yields are good. Results are consistent with the couple MnO2 / PyHF acting as a precursor of manganese (IV) tetrafluoride formed in situ.
  • Open access
  • 28 Reads
Substituted Pyrazinecarboxamides: Preparation and Biological Activity
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Newly synthesised pyrazinamide analogues with carboxamide moiety as a bridging ligands between basic and aromatic areas of molecule were tested for their antifungal and photosynthesis-inhibiting activity. The synthetic approach, analytical and spectroscopic data of all newly synthesized compounds are presented. The highest antifungal effect (MIC < 62.5 µmol l-1) against Candida albicans, the most susceptible fungal strain tested, was found for 6-chloropyrazine-2-carboxylic acid (3-chlorophenyl)amide. The most active inhibitor of oxygen evolution rate in spinach chloroplasts was 5-tert-butyl-6-chloropyrazine-2-carboxylic acid (3-chlorophenyl)amide (IC50 = 47.0 µmol dm-3).
  • Open access
  • 72 Reads
Synthesis of 7-(10, 11-Dihydro-5H-dibenzo[a,d]-cyclo-hepten-5-ylamino)-heptanoicacid (Amineptine)
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This paper discribes the improved synthesis of 7-(10, 11-Dihydro-5H-dibenzo[a,d]cyclohepten-5-ylamino)-heptanoicacid (5) a synthetic, atypical tricyclic anti-depressant with central nervous system stimulating effects[1,2]. The synthesis was developed in context of the DrugMatrix[3] genomics project.