1493-23-8

Upstream product

• 460-00-4 1-Bromo-4-fluorobenzene 
• 540-36-3 para-difluorobenzene 
• 109-72-8 n-butyllithium 
• 352-34-1 4-fluoro-1-iodobenzene 
• 31600-88-1 m-methoxyphenyllithium 
• 14774-78-8 4-chlorophenyl lithium 
• 591-51-5 phenyllithium 
• 25077-87-6 3-chlorophenyllithium 
• 107337-71-3 3-fluorophenyllithium 
• 14101-14-5 (4-fluorophenyl)trimethyltin 

Downstream Products

• 22217-86-3 2-(4-fluorophenyl)-Δ¹-pyrrolidine 
• 98034-18-5 2,2-Bis-(4-fluoro-phenyl)-3-methyl-oxirane 
• 82144-12-5 1,1-bis-(4-fluorophenyl)-ethylene oxide 
• 184376-51-0 (1R,2R,3R,5S)-3-(4-Fluoro-phenyl)-8-methyl-2-(3-methyl-[1,2,4]oxadiazol-5-yl)-8-aza-bicyclo[3.2.1]octane 
• 220474-60-2 1-benzyl-3-(4'-fluorophenyl)pyrrolidine 
• 371-41-5 4-Fluorophenol 
• 862283-91-8 (3R,4s,5S)-1-benzyl-4-(4-fluorophenyl)-3,5-dimethylpiperidin-4-ol 
• 357927-03-8 (2S)-1-(4-fluorophenyl)-1-(2-fluoro-pyridin-4-yl)-1,2-propanediamine 
• 498538-99-1 (2S)-1-(4-fluorophenyl)-1-(1,5-naphthyridin-3-yl)-1,2-propanediamine 
• 851337-37-6 rac-2-(4-fluoro-phenyl)-cyclohexanol 
• 133472-27-2 4-fluorophenylzinc chloride 
• 113530-51-1 cis-PdMe(p-FC₆H₄)(PEt₂Ph)2 
• 115289-14-0 (η5-cyclopentadienyl)(η2-ethylene)(4-fluorophenyl)nickel 
• 97348-61-3 cis-(4-tert-butylphenyl)(4-fluorophenyl)bis(triphenylphosphane)platinum(II) 

Relevant academic research and scientific papers

Artemisinin and a series of novel endoperoxide antimalarials exert early effects on digestive vacuole morphology

Artermisinin and its derivatives are now the mainstays of antimalarial treatment; however, their mechanism of action is only poorly understood. We report on the synthesis of a novel series of epoxy-endoperoxides that can be prepared in high yields from simple starting materials. Endoperoxides that are disubstituted with alkyl or benzyl side chains show efficient inhibition of the growth of both chloroquine-sensitive and -resistant strains of Plasmodium falciparum. A trans-epoxide with respect to the peroxide linkage increases the activity compared to that of its cis-epoxy counterpart or the parent endoperoxide. The novel endoperoxides do not show a strong interaction with artemisinin. We have compared the mechanism of action of the novel endoperoxides with that of artemisinin. Electron microscopy reveals that the novel endoperoxides cause the early accumulation of endocytic vesicles, while artemisinin causes the disruption of the digestive vacuole membrane. At longer incubation times artemisinin causes extensive loss of organellar structures, while the novel endoperoxides cause myelin body formation as well as the accumulation of endocytic vesicles. An early event following endoperoxide treatment is the redistribution of the pH-sensitive probe LysoSensor Blue from the digestive vacuole to punctate structures. By contrast, neither artemisinin nor the novel endoperoxides caused alterations in the morphology of the endoplasmic reticulum nor showed antagonistic antimalarial activity when they were used with thapsigargin. Analysis of rhodamine 123 uptake by P. falciparum suggests that disruption of the mitochondrial membrane potential occurs as a downstream effect rather than as an initiator of parasite killing. The data suggest that the digestive vacuole is an important initial site of endoperoxide antimalarial activity. Copyright

Generation of Phosphonium Sites on Sulfated Zirconium Oxide: Relationship to Br?nsted Acid Strength of Surface -OH Sites

The reaction of (tBu)2ArP (1a-h), where the para position of the Ar group contains electron-donating or electron-withdrawing groups, with sulfated zirconium oxide partially dehydroxylated at 300 °C (SZO300) forms [(tBu)2ArPH][SZO300] (2a-h). The equilibrium binding constants of 1a-h to SZO300 are related to the pKa of [(tBu)2ArPH]; R3P that form less acidic phosphoniums (high pKa values) bind stronger to SZO300 than R3P that form more acidic phosphoniums (low pKa values). These studies show that Br?nsted acid sites on the surface of SZO300 are not superacidic.

A Rapid Injection NMR Study of the Reaction of Organolithium Reagents with Esters, Amides, and Ketones

Unexpectedly high rates of reaction between alkyllithium reagents and amides, compared to esters and ketones, were observed by Rapid Inject NMR and competition experiments. Spectroscopic investigations with 4-fluorophenyllithium (ArLi, mixture of monomer and dimer in THF) and a benzoate ester identified two reactive intermediates, a homodimer of the tetrahedral intermediate, stable below -100°C, and a mixed dimer with ArLi. Direct formation of dimers suggested that the ArLi dimer may be the reactive aggregate rather than the usually more reactive monomer. In contrast, RINMR experiments with ketones demonstrated that the ArLi monomer was the reactive species. (Chemical Equation Presented).

Relative basicities of ortho-, meta-, and para-substituted aryllithiums

(Chemical Equation Presented) The relative basicities of aryllithiums bearing methoxy, chlorine, fluorine, trifluoromethyl and trifluoromethoxy substituents at the ortho, meta, and para positions have been assessed. To this end, two aryllithiums of compar

STEREOSELECTIVE SYNTHESIS OF 17-α -AND 17-β -ARYL STEROIDAL COMPOUNDS

A process for forming one or the other of a 17-α-aryl or 17-β-aryl steroidal compound in diastereo excess is disclosed. The process utilizes a 17-keto steroid to form a Δ16-17-aryl-steroid compound or a 17-β-hydroxy-17-α-aryl steroid compound that are reduced or deoxygenated, respectively, in the presence of Raney nickel to form a 17-β-aryl- steroid or 17-α-aryl steroid, respectively, in a diastereo ratio of at least 3:1.

Stannylated polynorbornenes as new reagents for a clean stille reaction

New functionalized polynorbornenes have been obtained in good yields by vinylic copolymerization of norbornene with a (norbornenyl)Sn-Bu2Cl monomer, catalyzed by [Ni(C6F5)2(SbPh 3)2]. Subsequent functionalization produces a wide variety of polymers with different -SnBu2R groups (R = aryl, vinyl, alkynyl). The polymers can be used as R-transfer reagents in Stille couplings, thereby providing easy workup and separation of the polymeric tin byproducts from the coupling products. Tin contents of around 0.05 wt% are found in the Stille products. The stannylated polymers can be recycled and reused with good efficiency.

Anthracene Derivative, and Light Emitting Element, Light Emitting Device, Electronic Device Using Anthracene Derivative

A novel anthracene derivative represented by General Formula (1) is provided, which enables the production of a light-emitting element with high luminous efficiency and a long lifetime. A high-performance light-emitting device and electronic device in which the anthracene derivative is employed are also disclosed. The anthracene derivative of the present invention is represented by General Formula (1), in which the unit A represents any one of substituents represented by General Formulae (1-1) to (1-3). The variables shown in Formulae (1) and (1-1) to (1-3) are defined in the specification.

PROCESS FOR THE PREPARATION OF N-[4-(4-FLUOROPHENYL)-5-FORMYL-6-ISOPROPYL-PYRIMIDIN-2-YL]-N-METHYLMETHANESULFONAMIDE

The present invention is directed to a method for the preparation of N-[4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl]-N-methylmethanesulfonamide and its use in the preparation of rosuvastatin or a pharmaceutically acceptable salt thereof.

Pharmaceutically active compounds

The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein and especially to selective MCR4 agonist compounds, to

METHOD FOR THE ORGANOMETALLIC PRODUCTION OF ORGANIC INTERMEDIATE PRODUCTS BY HALOGEN-METAL EXCHANGE REACTIONS

The invention relates to a method for producing aryllithium compounds and to their reaction with suitable electrophiles to obtain compounds of formula (V), by reacting halogen aromatics (I) with lithium metal to obtain an aromatic lithium compound (II), which, as a lithiation agent, reacts with aromatic halogen compounds (III) in a halogen-metal exchange reaction to form the corresponding lithium aromatics (IV). Said aromatics can be reacted in an additional step with a corresponding electrophile to form the desired product (V). Said method is illustrated by equation (I), in which Ar represents phenyl, pyridyl or naphthyl, which are optionally substituted with a radical from the group consisting of methyl, primary, secondary or tertiary alkyl, cycloalkyl, phenyl, substituted phenyl, aryl, heteroaryl, alkoxy, dialkylamino, alkylthio, fluoro, bromo; Hal1 = fluorine, chlorine, bromine or iodine, Hal2 = chlorine, bromine or iodine; the groups X1-5 independently of one another represent either carbon, or the group XiRi (i = 1-5) represents nitrogen, or two respective adjacent groups XiRi, linked by a formal double bond, together represent O (furane), S (thiophene), NRH or NRi (pyrroles). The groups R1-5 represent substituents from the group containing hydrogen, methyl, primary, secondary or tertiary, cyclic or acyclic alkyl groups with 2 to 12 C atoms, in which optionally one or more hydrogen atoms are replaced by fluorine or chlorine, e.g. CF3, substituted cyclic or acyclic alkyl groups, alkoxy, dialkylamino, alkylamino, arylamino, diarylamino, phenyl, substituted phenyl, heteroaryl, substituted heteroaryl, alkylthio, arylthio, diarylphosphino, dialkylphosphino, alkylarylphosphino, dialkyl-, arylalkyl- or diarylaminocarbonyl, monoalkyl- or monoarylaminocarbonyl, CO2-, alkyl- or aryloxycarbonyl, hydroxyalkyl, alkoxyalkyl, fluorine or chlorine, nitro, cyano, aryl- or alkylsulphone, aryl- or alkylsulphonyl, or two respective groups R1-5 together can represent an aromatic, heteroaromatic or aliphatic fused ring.