84772-30-5Relevant academic research and scientific papers
EXPERIMENTAL ANTIULCER AGENTS: N-SUBSTITUTED 2-(4-METHYL-1-PIPERAZINYL)ACETAMIDES AS PIRENZEPINE MODELS AND SOME RELATED COMPOUNDS
Hulinska, Hana,Polivka, Zdenek,Jilek, Jiri,Sindelar, Karel,Holubek, Jiri,et al.
, p. 1820 - 1844 (2007/10/02)
Reactions of N-cyclohexyl-2-chloroacetamide, N-phenyl-2-chloroacetamide, N-(4-dimethylaminophenyl)-2-chloroacetamide, N-(2-nitrophenyl)-N-phenyl-2-chloroacetamide, its 3-nitrophenyl and 4-nitrophenyl analogues, N-(2-benzylphenyl)-2-chloroacetamide, 5-(chloroacetyl)dibenzazepine, and its 10,11-dihydro derivative with piperazine, 1-methylpiperazine, 2-(1-piperazinyl)ethanol, and 3-(1-piperazinyl)propanol resulted in compounds II, III, V -XV, XVIII, XXI, and XXIII, simple analogues of the antiulcer agent pirenzepine (I).Contributions to the syntheses and characterization of mianserin (XIX), bisnor analogue of imipramine (XXV), and pirenzepine (I) are presented.Two 2-aryl-2-(2-pyridyl)thioacetamides XXXVIII and XL were synthesized via nitriles XXXIX and XLI.Compounds XI (VUFB-17 104) and XXI (VUFB-17 113) were found to be rather effective as anti-ulcer agents and anticholinergics.
Novel synthesis of 5,11-dihydro-6H-pyrido[2,3-b]-[1,4]-benzodiazepin-6-ones and related studies (1)
Oklobdzija,Comisso,Decorte,et al.
, p. 1329 - 1334 (2007/10/02)
5,11-Dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one (1), a basic intermediate in the preparation of 11-α-aminoacetyl derivatives with important biological activities, has been obtained by a three-step synthesis starting from easily available isatoic anhydride and anhydro ornithine. Some model cyclisation reactions leading to 5-member ring derivatives 10 and 12 instead of 7-member ring analogues of 1, are reported. Easy transformations of the tetrahydro congener of 1, i.e. compound 4 into 19, which actually represents a tetrahedral intermediate in the transformation of 5 into 4, is noticed. Further rearrangement of 19 into spiro compounds 20, and return of the latter into 5 is described.
