7056-72-6

Upstream product

• 141-82-2 malonic acid 
• 90-04-0 2-methoxy-phenylamine 
• 1663-67-8 malonoyl dichloride 
• 108-59-8 malonic acid dimethyl ester 
• 105-53-3 diethyl malonate 
• 90475-72-2 2-methoxymalonanilic acid ethyl ester 

Downstream Products

• 1614221-79-2 3,3-dibenzyl-4-hydroxy-8-methoxy-3,4-dihydro-1H-quinolin-2-one 
• 1614221-53-2 3,3-dibenzyl-8-methoxy-1H-quinoline-2,4-dione 
• 90475-69-7 3,3-Dichloro-8-methyl-2,4-dioxo-1,2,3,4-tetrahydroquinoline 

Relevant academic research and scientific papers

Designer ligands. VIII. Thermal and microwave-assisted synthesis of silver(I)-selective ligands

Thermal and microwave-assisted methods have been used for preparing multidentate malonamide derivatives as silver(I)-selective ligands, the latter methodology providing convenient and rapid access to the target compounds in yields of up to 92%. Metal extr

Synthesis of 6-methoxy-N 2,N 2,N 4,N 4,N 5,N 5-hexamethylquinoline-2,4,5-triamine - A new representative of quinoline proton sponges

[Figure not available: see fulltext.] We report the synthesis of 4-chloro-2-methyl-5-nitro- and 2,4-dichloro-5-nitroquinolines, containing methoxy groups at positions 6 and 8. The reaction of these compounds with dimethylamine solution in alcohol was shown to produce not only aminodehalogenation products, but also resulted in nucleophilic substitution of the methoxy groups. The reduction of 6-methoxy-N 2,N 2,N 4,N 4-tetramethyl-5-nitroquinoline-2,4-diamine with subsequent methylation gave 6-methoxy-N 2,N 2,N 4,N 4,N 5,N 5-hexamethylquinoline-2,4,5-triamine, a new representative of quinoline proton sponges.

Synthesis of symmetrically substituted 3,3-dibenzyl-4-hydroxy-3,4-dihydro- 1H-quinolin-2-ones, as novel quinoline derivatives with antibacterial activity

A novel series of symmetrically substituted 3,3-dibenzyl-4-hydroxy-3,4- dihydro-1H-quinolin-2-ones was synthesized and tested as antimicrobials. The minimum inhibitory concentration (MIC) values of the most active heterocycles were slightly higher than those exhibited by levofloxacin, employed as comparator. Structural factors affecting the activity were explored along three diversification points, including the substituents of the aromatic rings of the 3-benzyl moieties, as well as the functionalization of both, the homocyclic ring of the heterocycle and the quinolonic nitrogen atom. 6-Chloro and 3,3-bis(4′-chlorobenzyl) derivatives showed the lower MIC values. Optimally substituted heterocycles were synthesized, which exhibited enhanced activity.

Ligand-based modelling followed by synthetic exploration unveil novel glycogen phosphorylase inhibitory leads

Glycogen phosphorylase (GP) is a valid anti-diabetic target. Accordingly, we applied a drug discovery workflow to unveil novel inhibitory GP leads via combining pharmacophore modeling, QSAR analysis and in silico screening, followed by synthetic exploration of active hits. Virtual screening identified six low micromolar inhibitory leads from the National Cancer Institute (NCI) list of compounds. The most potent hits exhibited anti-GP IC50 values of 3.2 and 4.1 μM. Synthetic exploration of hit 59 (IC50 = 4.1 μM) yielded 25 lead inhibitors with the best illustrating IC50 of 3.0 μM. Interestingly, we prepared several novel mixed oxalyl amide anti-GP leads employing new chemical reaction involving succinic acid-based adducts.

Design and synthesis of bis-amide and hydrazide-containing derivatives of malonic acid as potential HIV-1 integrase inhibitors

HIV-1 integrase (IN) is an attractive and validated target for the development of novel therapeutics against AIDS. In the search for new IN inhibitors, we designed and synthesized three series of bis-amide and hydrazide-containing derivatives of malonic acid. We performed a docking study to investigate the potential interactions of the title compounds with essential amino acids on the IN active site.

Ethyl Esters of Malonanilic Acids. Synthesis and Pyrolysis

The pyrolysis under 170-220 deg C or boiling in DMF of malonanilic acids ethyl esters (2) is accompanied by formation of malonic acids symmetric dianilides (7) with high yields.A possible mechanism for this transformation has been suggested.

A CONVENIENT APPROACH TO THE SYNTHESIS OF PRENYL-, FURO- AND PYRANO-QUINOLINE ALKALOIDS OF THE RUTACEAE

A convenient method for the synthesis of 4-hydroxy-3-prenyl-2-quinolones, wjich have been recognised as precursors to prenyl-, furo- and pyranoquinoline alkaloids of the Rutaceae is described.The methodology involves C,C-diprenylation of 2,4-dihydroxyquinoline followed by partial deallylation using sodium hydrogen telluride reagent.

Synthesis of Swietenidin-A Methyl Ether

Swietenidin-A methyl ether has been synthesised starting from o-anisidine and diethyl malonate