M. Anil Kumar

Stereoselective synthesis of artemisinin

Abstract A stereoselective synthesis of artemisinin 11 based on intramolecular Diels-Alder reaction of the triene 4 derived from (+)isolimonene 2 is described.

PEG-SO3H catalyzed synthesis and cytotoxicity of α-aminophosphonates

One pot three-component PEG-SO(3)H catalyzed reaction of 4-(Pyridin-4-yl)benzaldehyde and triethyl phosphite with various primary amines afforded α-aminophosphonates with high yields by the Kabachnik-Fields reaction. These new structurally diversified set of α-aminophosphonates (4a-j) were evaluated for their anti-tumor activity on human chronic myeloid leukemia cells (K 562), human colon carcinoma cells (Colo 205) along with non-cancerous human embryonic kidney cells (HEK 293). They showed moderate activity on both cancerous cells and non-cancerous cells.

Synthesis and bio-activity evaluation of tetraphenyl(phenylamino) methylene bisphosphonates as antioxidant agents and as potent inhibitors of osteoclasts in vitro.

A new series of tetraphenyl bisphosphonates have been elegantly synthesized by one-pot method and were characterized by elemental analysis, FTIR, 1H, 13C, 31P NMR, mass spectra and evaluated for their in vitro antibone resorptive activity by inhibiting growth of osteoclasts. Two bisphosphonates 3g and 3f showed marked inhibition ratio (8 μM and 10 μM) and emerged as lead compounds. All compounds were tested for their antioxidant (DPPH scavenging, reducing power and inhibition of lipid peroxidation). They exhibited potent in vitro antioxidant activity dose-dependently.

Stereospecific synthesis of α-lipoic acid

Abstract Short and highly stereospecific synthesis of (S)-(-)- and (R)-(+)-α-lipoic acid using menthone as a recyclable chiral auxiliary is presented.

Phosphomolybdic Acid/SiO2 as Heterogeneous Solid Acid Catalyst for the Rapid Synthesis of N-Substituted Pyrroles

Abstract Isatins react efficiently with 4-hydroxyproline in the presence of 10 mol% of PMA/SiO2 in acetonitrile/water (4:1) under reflux conditions to furnish N-substituted pyrroles in excellent yields. Similarly, 11H-indeno[1,2-b]quinoxalin-11-ones also participated in this reaction.

Oxone as a Mild, Inexpensive, and Environmentally Benign Oxidant for the α-Thiocyanation of Ketones

Abstract An efficient and direct approach for the α-thiocyanation of ketones with α-hydrogens has been developed using ammonium thiocyanate as a thiocyanating agent and oxone as an oxidant in methanol.

Synthesis and Antimicrobial Activity of 1‐[(Substituted Carbamoyl)Amino]‐1H,3H‐1λ5‐[1,3,2]oxazaphospholo[3,4‐a]benzimidazol‐1‐ones

Abstract 1‐[(Substituted carbamoyl)amino]‐1H,3H‐1λ5‐[1,3,2]oxazaphospholo[3,4‐a]benzimidazol‐1‐ones were synthesized by reacting benzimidazole 2‐methanol (4) with different chlorides of carbamidophosphoric acids (3) in the presence of triethylamine at 40–45°C. Their 1H, 13C, and 31P NMR spectral data were discussed. The title compounds were tested for their activity against the fungi Aspergillus niger and Fusarium solani and bacteria Staphylococcus aureus and Escherichia coli. These compounds showed moderate antibacterial activity when compared with antifungal activity.