24302-10-1

Upstream product

• 5292-53-5 diethyl benzalmalonate 
• 124-38-9 carbon dioxide 
• 100-52-7 benzaldehyde 
• 105-53-3 diethyl malonate 

Downstream Products

• 934619-05-3 (E)-2-(4-fluorobenzylcarbamoyl)-3-phenylacrylic acid ethyl ester 
• 1846-76-0 ethyl coumarin-3-carboxylate 
• 130734-36-0 2-methyl-6-oxo-4-phenyl-1,4,5,6-tetrahydropyridine-3-carboxylic acid methyl ester 
• 77416-50-3 (E)-2-(Benzyloxycarbonyl-methyl-amino)-3-phenyl-acrylic acid ethyl ester 
• 77416-51-4 (Z)-2-(Benzyloxycarbonyl-methyl-amino)-3-phenyl-acrylic acid ethyl ester 
• 72015-61-3 (Z)-2-benzyloxycarbonylaminocinnamic acid 
• 77416-48-9 (Z)-2-Azidocarbonyl-3-phenyl-acrylic acid ethyl ester 
• 52157-07-0 (E)-2-Isocyanato-3-phenyl-acrylic acid ethyl ester 
• 50685-13-7 ethyl (Z)-α-N-benzyloxycarbonyl-α,β-didehydrophenylalaninate 
• 50685-12-6 N-<(Carbobenzyl)oxy>-Δ^E-phenylalanine Ethyl Ester 
• 934619-04-2 2-benzylidene-N-(4-phenyl-butyl)-N'-trityloxy-malonamide 
• 934619-07-5 2-benzylidene-N-(4-fluoro-benzyl)-N'-trityloxy-malonamide 
• 934619-03-1 2-benzylidene-N-(4-fluoro-benzyl)-N'-trityloxy-malonamide 
• 934619-01-9 (Z)-3-phenyl-2-trityloxycarbamoylacrylic acid ethyl ester 

Relevant academic research and scientific papers

Copper-Catalyzed Carboxylation of C-F Bonds with CO2

An effective Cu-catalyzed selective formal carboxylation of C-F bonds with an atmospheric pressure of CO2 is reported. A variety of gem-difluoroalkenes, gem-difluorodienes, and α-trifluoro-methyl alkenes show high reactivity and selectivity for

Synthesis of coumarins via PIDA/I2-mediated oxidative cyclization of substituted phenylacrylic acids

A variety of functionalized coumarins were synthesized from substituted phenylacrylic acids via PIDA/I2-mediated and irradiation-promoted oxidative carbon-oxygen bond formation. Our studies show that the oxygen in the pendant carboxylic acid group cyclizes favorably to the aryl ring that is cis to it. The main advantages of this method include good functional group tolerance and the transition-metal-free characteristic. The Royal Society of Chemistry 2013.

Hydroxamates: Relationships between structure and plasma stability

Hydroxamates are valuable tools for chemical biology as well as interesting leads for medicinal chemistry. Although many hydroxamates display nanomolar activities against metalloproteases, only three hydroxamates have reached the market, among which is the HDAC inhibitor vorinostat. Failures in development are generally attributed to lack of selectivity, toxicity, or poor stability. To help medicinal chemists with respect to plasma stability, we have performed the first and preliminary study on structure-plasma stability for hydroxamates. We define some structural rules to predict or improve the plasma stability in the preclinical stage.

Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents

Proteases that are expressed during the erythocytic stage of Plasmodium falciparum are newly explored drug targets for the treatment of malaria. We report here the discovery of potent inhibitors of PfA-M1, a metallo- aminopeptidase of the parasite. These

Synthesis of polysubstituted 1,3-cyclohexadicnes from β-branched α,β-alkenals and monoesters of ylidenemalonic acids

3-Methyl- and 3-phenyl-2-butenal react with monoesters of alkylidene-, alkenylidene-, and arylmethylenemalonic acids in the presence of piperidine as the catalyst to give esters of 4,6-disubstituted 1,3-cyclohexadienecarboxylic acids in 23-96 % yields. Under the same conditions cyclohexylideneacetic aldehyde reacts with the monoesters of prenylidene- and benzylidenemalonic acid to afford mixtures of 1,8a-trans- and 1,8a-cis-isomers of 1-substituted alkyl 1,5,6,7,8,8a-hexahydronaphthalene-2-carboxylates, the ratios and configurations of which were determined by means of 1H NMR spectroscopy. In some cases the formation of cyclic dienes is impeded by the competing process of decarboxylation of acidic ylidenemalonates. The derivatives of 4,6-diphenyl-1,3-cyclohexadienecarboxylic acid were shown to be convenient precursors for the preparation of meta-terphenyls.

Steric and electronic requirements of amide and ester groups in benzylidenemalonates

Stereoisomeric benzylidinemalonates have been synthesised. In the case of N-(2-ethoxycarbonyl-3-phenylpropenoyl)-2-oxazolidinone, both E- and Z-isomers could be obtained, but the Z-isomer isomerised (> 95%) to the E-isomer in the presence of catalytic amo

Enzyme-Catalyzed Hydrolyses of E/Z-Diastereotopic and E/Z-Diastereomeric Esters. Affect on Selectivity by Reaction Media

PLE-catalyzed hydrolyses of different types of E/Z-diastereotopic diesters and E/Z-diastereomeric monoesters have been studied.Arylidenepropanedioic diesters are specifically hydrolyzed to the Z-half esters, whereas the de values for dialkylated methylene propanedioic diesters range between 33 and 79percent (Z).D values for the hydrolyses of the 3-methyleneazetidin-2-ones in detergent-buffer systems depend on the size of the substituent in the α-position.Diastereoselectivity of these substrates is affected by addition of the cosolvents acetonitrile and methanol.

N--ΔE-phenylalanine Ethyl Ester

The synthesis of the title compound (1a) has been accomplished by rearrangement of a vinylic isocyanate, and its configuration was confirmed by X-ray crystallography.The configurational stability of 1a to both acids and bases was investigated, and the NMR