Highly efficient syntheses of novel fluorine bearing quinoline-4-carboxylic acids and the related compounds had been achieved from cyclocondensation of 2-amino-5-fluorophenyl glyoxylic acid 1 with benzoyle asetanilide...Highly efficient syntheses of novel fluorine bearing quinoline-4-carboxylic acids and the related compounds had been achieved from cyclocondensation of 2-amino-5-fluorophenyl glyoxylic acid 1 with benzoyle asetanilides 2 in boiling DMF, to give the target 3. Decarboxylation of 3 produced 6-fluoro-2-phenyl-3-(substituted amino)-keto-quinolines 4, while that reaction underwent refluxing, afforded 7-fluoro-1-(aryl)-3-phenyl-pyrrolo[3,4-c] quinoline-2,9-diones 5. Structure of the products has been established from their elemental and spectral analysis. All targets exhibited a high to moderate activity against some Aspergillus fungi as amylolytic agents.展开更多
Pyrazoles are important nitrogen containing 5-membered heterocyclic compounds. Numerous pyrazoline derivatives have been found to possess considerable biological activities, which stimulated the research activity in t...Pyrazoles are important nitrogen containing 5-membered heterocyclic compounds. Numerous pyrazoline derivatives have been found to possess considerable biological activities, which stimulated the research activity in this field. Several 1,3,5-Triphenyl-1H-pyrazole containing 6-aminopyridazin-3(2H)-one derivatives has been synthesized. These new compounds were characterized using IR, 1H-NMR and Mass spectra and Elemental analysis. They possess some potent biological activities. Therefore biological screening of novel compounds has been also done.展开更多
An efficient synthesis of substituted 1,3-dihydroisobenzofurans is developed. In this novel route, oaroylbenzaldehydes, as key intermediates, can be obtained by lead tetraacetate oxidation of Naroylhydrazones of salic...An efficient synthesis of substituted 1,3-dihydroisobenzofurans is developed. In this novel route, oaroylbenzaldehydes, as key intermediates, can be obtained by lead tetraacetate oxidation of Naroylhydrazones of salicylaldehydes. The mild and general strategy enables the synthesis of various substituted 1,3-dihydroisobenzofurans in high yields. Moreover, this method can be applied to efficiently synthesize escitalopram.展开更多
文摘Highly efficient syntheses of novel fluorine bearing quinoline-4-carboxylic acids and the related compounds had been achieved from cyclocondensation of 2-amino-5-fluorophenyl glyoxylic acid 1 with benzoyle asetanilides 2 in boiling DMF, to give the target 3. Decarboxylation of 3 produced 6-fluoro-2-phenyl-3-(substituted amino)-keto-quinolines 4, while that reaction underwent refluxing, afforded 7-fluoro-1-(aryl)-3-phenyl-pyrrolo[3,4-c] quinoline-2,9-diones 5. Structure of the products has been established from their elemental and spectral analysis. All targets exhibited a high to moderate activity against some Aspergillus fungi as amylolytic agents.
文摘Pyrazoles are important nitrogen containing 5-membered heterocyclic compounds. Numerous pyrazoline derivatives have been found to possess considerable biological activities, which stimulated the research activity in this field. Several 1,3,5-Triphenyl-1H-pyrazole containing 6-aminopyridazin-3(2H)-one derivatives has been synthesized. These new compounds were characterized using IR, 1H-NMR and Mass spectra and Elemental analysis. They possess some potent biological activities. Therefore biological screening of novel compounds has been also done.
基金supported by the National Basic Research Program of China(No.2011CB933503)Technology Supporting Program of Jiangsu Province(Nos.BE2009639 and BE2012657)
文摘An efficient synthesis of substituted 1,3-dihydroisobenzofurans is developed. In this novel route, oaroylbenzaldehydes, as key intermediates, can be obtained by lead tetraacetate oxidation of Naroylhydrazones of salicylaldehydes. The mild and general strategy enables the synthesis of various substituted 1,3-dihydroisobenzofurans in high yields. Moreover, this method can be applied to efficiently synthesize escitalopram.
