Synthesis of fluorinated spiro-1,3-oxazines and thiazines Selectfluor-mediated intramolecular cyclization.

A fluorination-induced intramolecular cyclization for the synthesis of fluoro-substituted spiro-1,3-oxazine and spiro-1,3-thiazine derivatives is described. -(2-(Cyclohex-1-en-1-yl)ethyl)benzamide and benzothioamide are used as the substrates, and the cationic fluorinating agent Selectfluor works as the fluoride source. The reaction yields a single diastereomer.

Copper-catalysed dehydrogenative self-coupling/cyclization of 5-aminopyrazoles: synthesis and photophysical study of pyridazines.

An interesting self-coupling/cyclization of 5-aminopyrazoles is revealed, which provides a variety of pyridazine cores in reasonable yields. In this reaction, C(sp)-C(sp) and N-N bond formation occurs simultaneously in one reaction vessel. The photophysical properties of the synthesized compounds were also studied and some of them exhibited fluorescence properties with good quantum yields.

Ten Years of Glory in the α-Functionalizations of Acetophenones: Progress Through Kornblum Oxidation and C-H Functionalization.

This review article focuses on the α-functionalization of acetophenones involving Kornblum oxidation and C-H functionalizations. Although various other strategies, such as classical approaches, enamine approaches and umpolung strategy are also known for this functionalization, here we discuss mainly the Kornblum oxidation approach and C-H functionalization strategy as they have advantages over the others. In Kornblum oxidation, the reaction uses iodine and dimethylsulfoxide and proceeds through the formation of arylglyoxal as the key intermediate.

Bioassay-guided isolation of potent α-glucosidase inhibitory compounds from the fruit of Buch-Ham ex D Don. and their screening.

Two bioactive compounds caffeic and sinapic acid were isolated from the fruit of the Buch-Ham ex D Don using bioassay guided approach. These compounds were isolated from water fraction using column chromatography followed by semi preparative HPLC. These compounds showed very potent anti-diabetic and antioxidant activities.

An expedient approach to 1,2-dihydroisoquinoline derivatives via cobalt catalysed 6-endo dig cyclization followed by Mannich condensation of o-alkynylarylaldimines.

A highly effective 6-endo dig cyclisation of o-alkynylaldimines to 1,2-dihydroisoquinolines has been described via direct and nitro Mannich condensation using inexpensive and readily available cobalt chloride as catalyst. This strategy provides an effective procedure for the synthesis of substituted 1,2-dihydroisoquinolines derivatives in moderate to high yields. An addition of pronucleophiles, such as nitromethane, acetone and α-hydroxyacetone, to o-alkynylarylaldimines has been achieved via isoquinolinium intermediate.

Bi and tri-substituted phenyl rings containing bisbenzimidazoles bind differentially with DNA duplexes: a biophysical and molecular simulation study.

Recently synthesis of programmable DNA ligands which can regulate transcription factors have increased the interest of researchers on the functional ability of DNA interacting compounds. A series of DNA interacting compounds are being designed which can differentiate between GC and AT rich DNA. In this study, we have studied the specificity of a few novel bisbenzimidazoles having different bi/tri-substituted phenyl rings, with DNA duplexes using spectroscopic methods.