118267-62-2

Upstream product

• 141-97-9 ethyl acetoacetate 
• 89-99-6 2-fluorobenzylamine 
• 506-87-6 ammonium carbonate 
• 446-52-6 2-Fluorobenzaldehyde 

Downstream Products

• 940565-36-6 diethyl 2,6?dimethyl?4?(o?fluorophenyl)pyridine?3,5?dicarboxylate 

Relevant academic research and scientific papers

Magnesium nitride as a convenient source of ammonia: preparation of dihydropyridines

(Chemical Equation Presented) Magnesium nitride (Mg3N 2) has been investigated for the preparation of dihydropyridines. This is a commercially available, bench-stable solid that generates ammonia upon treatment with protic solvents. The main features of the process are the facile reaction setup and good yields obtained in the majority of cases.

Urea as an ammonia surrogate in the hantzsch’s synthesis of polyhydro-quinolines / 1,4-dihydropyridines under green reaction conditions

Synthesis of polyhydroquinolines via Hantzsch’s multicomponent reaction (MCR) involves the use of a hygroscopic and moderately toxic ammonium salt as one of the key reactants. In our effort, we have found urea as an effective ammonia surrogate when the MC

Metal free biomimetic deaminative direct C-C coupling of unprotected primary amines with active methylene compounds

An unprecedented direct C-C coupling reaction of unprotected primary amines with active methylene compounds is reported. The reaction involves a biomimetic deamination of amines which was achieved under conditions free of metallic reagents and strong oxidizing agents. A wide range of primary amines was reacted with different active methylene compounds to provide structurally diverse trisubstituted alkenes and dihydropyridines. A kinetic study revealed an activation barrier of 10.1 kcal mol-1 for the conversion of a key intermediate of the reaction.

Air-stable zirconocene bis(perfluorobutanesulfonate) as a highly efficient catalyst for synthesis of N-heterocyclic compounds

Zirconocene bis(perfluorobutanesulfonate) is air- and water-stable and proved to be ionic on basis of conductivity measurements. It exhibits high catalytic efficiency for the synthesis of N-heterocyclic compounds under solvent-free condition, such as benzimidazoles, benzodiazepines, dihydropyrimidinones and dihydropyridines under mild condition. Furthermore, it can be reused without loss of activity in a test of five cycles. This catalytic system affords a simple and efficient approach for the synthesis of N-heterocyclic compounds.

One-Pot Three-Component Synthesis of Hantzsch 1,4-Dihydropyridines Promoted by Dimethyl Phosphate Ionic Liquids

A one-pot three-component reaction of ethyl acetoacetate, AcONH4, and different aldehydes has been successfully performed in the presence of ionic liquids (ILs) possessing a (MeO)2PO2- counterion. The impact of electronic and steric effects of the substituents of aromatic aldehydes, as well as the influence of different anions of ILs on the product yield, have been investigated. The application of dimethyl phosphate ILs in the synthesis of Hantzsch 1,4-dihydropyridines presents a simple method for obtaining structurally diverse products in moderate to high yields without using any additional catalyst.

Synthesis of diethyl 4-substituted-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylates as a new series of inhibitors against yeast α-glucosidase

1,4-Dihydropyridine-3,5-dicarboxylate derivatives (1-25) were synthesized in high yields via Hantzsch reaction and evaluated for their α-glucosidase inhibitory activity. Compounds 1, 2, 6-8, 11, 13-15, and 23-25 showed a potent inhibitory activity against yeast α-glucosidase with IC50 values in the range of 35.0-273.7 μM, when compared with the standard drug acarbose (IC50 = 937 ± 1.60 μM). Their structures were characterized by different spectroscopic techniques. The kinetics, selectivity, and toxicity studies on these compounds were also carried out. The kinetic studies on most active compounds 14 and 25 determined their modes of inhibition and dissociation constants Ki. Compound 14 was found to be a non-competitive inhibitor with Ki = 25.0 ± 0.06, while compound 25 was identified as a competitive inhibitor with Ki = 66.0 ± 0.07 μM.

Silica (NPs) supported Fe (III) as a reusable heterogeneous catalyst for the one-pot synthesis of 1, 4-dihydropyridines under mild conditions

A cheap and recyclable silica (NPs) supported Fe (III) was prepared as heterogeneous catalyst for the synthesis of various substituted 1,4-dihydropyridines via condensation of aldehydes with ethyl acetoacetate and ammonium acetate in ethanol. The products

COMPOUNDS AND COMBINATIONS THEREOF FOR INHIBITING BETA-AMYLOID PRODUCTION AND METHODS OF USE THEREOF

Provided are compounds which can be used in combination for treating diseases associated with a condition associated with cerebral accumulation of Alzheimer’s amyloid, such as Alzheimer’s disease. Also provided are methods of treating or reducing the risk of developing β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer’s amyloid by administering therapeutically effective amounts of compounds which in combination can decrease β-amyloid production and capacitative calcium entry in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer’s amyloid in animals or humans by administering diagnostically effective amounts of the compounds.