61875-53-4Relevant articles and documents
N-arylacetyl thiosemicarbazide urease inhibitor and preparation method and application thereof
-
Paragraph 0027-0028, (2019/01/14)
N-arylacetyl thiosemicarbazide compounds have a structural formula as shown in the specification, have great inhibiting effects on urease and can be used for preparation of medicines for treating gastritis, gastric ulcer, lithangiuria and the like. The in
Synthesis of Unsymmetrical Diaryl Acetamides, Benzofurans, Benzophenones, and Xanthenes by Transition-Metal-Free Oxidative Cross-Coupling of sp3 and sp2 C-H Bonds
Rathore, Vandana,Sattar, Moh.,Kumar, Raushan,Kumar, Sangit
, p. 9206 - 9218 (2016/10/14)
A chemo- and regioselective intermolecular sp3 C-H and sp2 C-H coupling reaction for C-C bond formation is described to access unsymmetrical diaryl acetamides under TM-free conditions from sec- and tert-arylacetamides and nitroarenes using tert-butoxide base in DMSO at room temperature. The coupling partners with sensitive functionalities such as chloro, bromo, hydroxy, and cyano were also amenable to the developed reaction. Synthesized α-(2/4-nitroaryl) phenylacetamides have been transformed into biologically important benzofurans, xanthenes, diaryl indoles, and unsymmetrical benzophenones by novel routes without applying a transition metal. Overall, an economical, yet efficient, strategy has been devised to access unsymmetrical diarylacetamides with the possibility of their further elaboration into a variety of biologically important heterocycles. Mechanistic understanding suggests that the reaction proceeds by a nucleophilic addition of a phenylacetamide carbanion, which is generated in the presence of tert-butoxide base, to the para or ortho (if para is substituted) position of nitrobenzene. The formed α-(4-nitrocyclohexa-2,4-dien-1-yl) phenylacetamide anion intermediate oxidized by a basic solution of DMSO or atmospheric oxygen led to the desired sp3 C-H and sp2 C-H coupled α-(2/4-nitroaryl) phenylacetamides.
AMINOPYRIDINE DERIVATIVES AS PLASMA KALLIKREIN INHIBITORS
-
Page/Page column 30, (2013/08/15)
The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.