Mild Brønsted basic ionic liquids catalyzed three component synthesis of pyrazolo[1,2-a][1,2,4]triazole-1, 3-dione and 2-amino-3-cyano-5,10-dioxo-4-phenyl-5, 10-dihydro-4H-benzo[g]chromene derivatives

Pyrazolo[1,2-a][1,2,4]triazole-1,3-dione derivatives were synthesized via a three component reaction of arylaldehydes, 4-phenylurazole and malononitrile in the presence of a catalytic amount of 2-hydroxyethylammonium formate and 2-hydroxyethylammonium acetate as effective mild basic ionic liquids, without using any additional co-catalyst, under solvent-free conditions at room temperature in good yields. Ionic liquids as catalysts were recovered and reused. In addition, the preparation of 2-amino-3-cyano-5,10-dioxo-4-phenyl-5,10-dihydro-4H-benzo[g]chromene derivatives from the reaction of arylaldehydes, malononitrile and 2-hydroxy-1,4-dihydronaphthalene-1,4-dione under solvent-free conditions at ambient temperature in the presence of mentioned catalysts is reported

Mild and Efficient Synthesis of Polysubstituted Phthalimides and Piperidines Catalyzed by DABCO

Polysubstituted phthalimide derivatives have been isolated in excellent yield from the addition reaction between acetoacetanilide and dialkyl acetylenedicarboxylates by using DABCO as an efficient basic catalyst in EtOH at room temperature. This procedure led to the formation of new phthalimide derivative in the presence of di-tert-butylacetylendicarboxylate as acetylenic ester. The methodology has also been applied successfully for the synthesis of novel piperidine substitutes via the simple reaction between acetoacetanilide and alkyl propiolates. These reactions have some advantages such as not only the process is eco-friendly but also the yields are good and the work-up is simple

Measurements of islet function and glucose metabolism with the dipeptidyl peptidase 4 inhibitor vildagliptin in patients with type 2 diabetes.

Objective: Pharmacological inhibition with the dipeptidyl peptidase 4 (DPP-4) inhibitor vildagliptin prolongs the action of endogenously secreted incretin hormones leading to improved glycemic control in patients with type 2 diabetes mellitus (T2DM). We undertook a double-blinded, randomized-order, crossover study to examine the vildagliptin mechanisms of action on islet function and glucose utilization. Research Design and Methods: Participants with T2DM (n 16) who had a baseline hemoglobin A1c of 7.1 0.2% completed a crossover study with 6 wk of treatment with vildagliptin and 6 wk with placebo. At the completion of each arm, participants had a study of postprandial metabolism and a two-step glucose clamp performed at 20 and 80 mU/minm2 insulin infusions. Results: Vildagliptin increased postprandial glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide by 3- and 2-fold, respectively, reduced fasting plasma glucose and postprandial plasma glucose by 1.3 0.3 mmol/liter and 1.6 0.3 mmol/liter (both P 0.01), and improved glucose responsiveness of insulin secretion by 50% (P 0.01). Vildagliptin lowered postprandial glucagon by 16%(P0.01). Examined by glucose clamp, insulin sensitivity and glucose clearance improved after vildagliptin (P 0.01). Conclusions: Vildagliptin improves islet function in T2DM and improves glucose metabolism in peripheral tissue