The aim of this work is to develop a simple, fast and efficient method for the synthesis optically pure enantiomers some 5-aryl-substituted 3-methyl‑7-nitro‑1,2-dihydro‑3H‑1,4-benzodiazepin‑2-ones using simple reagents. In course study, we found that interaction 2-amino‑5-nitrobenzophenone or 2-amino‑2’-chloro‑5-nitrobenzophenone with active L- D‑α-alanine N‑carboxyanhydrides in presence two eq...

The synthesis of the tetracyclic molecule 2-(9,10-dihydro-9,10-propano-anthracen-9-yl)-N-methylethanamine (2) as a homologue of the antidepressant 1-(9,10-dihydro-9,10-ethanoanthracen-9-yl)-N-methylmethaneamine (1) was described. The key intermediate 9-(prop-2-en-1-yl)-9,10-dihydro-9,10-propanoanthracen-12-one (7) was successfully synthesized via a [4+2] cycloaddition of alpha-bromoacrolein and...

Both the enantiomers of 2,3-dihydro-1,4-benzodioxin-2-carboxylic acid are valuable chiral synthons for enantiospecific synthesis of therapeutic agents such as (S)-doxazosin mesylate, WB 4101, MKC 242, 2,3-dihydro-2-hydroxymethyl-1,4-benzodioxin, and N-[2,4-oxo-1,3-thiazolidin-3-yl]-2,3-dihydro-1,4-benzodioxin-2-carboxamide. Pharmaceutical applications require these enantiomers in optically pure...

The crystal structures are reported for two unsubstituted arylnaphthalene lactones, 4-phenylnaphtho[2,3-c]furan-1(3H)-one (2), 9-phenylnaphtho[2,3-c]furan-1(3H)-one (3) and a non-aromatic dihydro arylnaphthene lactone, 3a,4-dihydro-9-phenylnaphtho[2,3-c]furan-1(3H)-one (5). There only minor differences in the geometrical parameters of these structures. However, certain cases, both isomers lacto...

The novel compound 2-(1H-imidazol-2-yl)-2,3-dihydro-1H-perimidine was obtained in very good yield via a known eco-friendly protocol. product isolated pure form as solvate by simple filtration from the crude mixture. Its structure assigned 1D and 2D NMR experiments confirmed high resolution MS single crystal XRD. temperature of methanol release determined DSC energy process theoretically estimat...

Abstract New convenient synthetic methods in pyrazoline and pyrazolooxazine chemistry have been developed starting from 2,2‐dichlorovinylacetophenones 4 , whose reaction with 2‐hydroxyethylhydrazine directly gave hitherto unknown 3‐aryl‐5‐dichloromethyl‐1‐(2‐hydroxiethyl)‐2‐pyrazolines 7 high yields. These were found to be able undergo cyclization afford 2‐aryl‐6,7‐dihydro‐4 H ‐pyrazolo[5,1‐ c ...