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Synthesis of a chiral fluorescence active probe and its application as an efficient catalyst in the asymmetric Friedel-Crafts alkylation of indole derivatives with nitroalkenes

Novel chiral Zn(ii) complexes were synthesized and these complexes showed fluorescence behaviour. These chiral Zn(ii) complexes were tested in the asymmetric Friedel-Crafts alkylation reaction of indole derivatives with nitroalkenes. In all the cases, the desired product was obtained with high yield (up to 93%) and good enantioselectivity (up to 78% ee) under the optimized reaction conditions. The effects of solvent, metallic salt and piperidine ratio on the fluorescence intensity of the catalyst and on the enantioselectivity of the desired products were discussed.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Final Thoughts on Chemistry for (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol

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Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity

Several imidazole-based cyclohexyl amides were identified as potent CB-1 antagonists, but they exhibited poor oral exposure in rodents. Incorporation of a hydroxyl moiety on the cyclohexyl ring provided a dramatic improvement in oral exposure, together with a ca. 10-fold decrease in potency. Further optimization provided the imidazole 2-hydroxy-cyclohexyl amide 45, which exhibited hCB-1 Ki = 3.7 nM, and caused significant appetite suppression and robust, dose-dependent reduction of body weight gain in industry-standard rat models.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

New explortion of 108-47-4

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Related Products of 108-47-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.108-47-4, Name is 2,4-Dimethylpyridine, molecular formula is C7H9N. In a Patent£¬once mentioned of 108-47-4

A direct catalytic oxidation process for synthesizing pyridine pergam amide compound method (by machine translation)

The present invention discloses a direct catalytic oxidation process for synthesizing pyridine pergam amide compound method, the under the action of acid or alkali, with formamide as carbonyl source and nitrogen source, the accelerator and water and oxidizing agent, in the silver and/or iron under the action of catalyst, pyridine or its derivative by catalytic oxidation of the carbon-hydrogen bond directly preparing pyridine pergam amide compound. Preparation of pyridine of the present invention method of primary amide compound, by the activation of the two-carbon-hydrogen bond, has an ideal atom economy and the advantages of less waste produced, substrate source is wide, stable and low price. Under the optimized reaction conditions, yield of a target product, separation of up to 98%. (by machine translation)

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Can You Really Do Chemisty Experiments About 126456-43-7

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POLYMORPHIC FORM OF A TACHYKININ RECEPTOR ANTAGONIST

This invention is concerned with a novel polymorphic forms of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethyl-amino)methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl) morpholine hydrochloride which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic forms have advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethylamino)methyl-1, 2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Top Picks: new discover of (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol

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Method of producing cis-1-aminoindan-2-ol

1,2-di-substituted indan expressed by general formula (I) wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, Y is a halogen atom, and X and Y can be in either cis- or trans-configuration forming either a racemic body or an optically active substance; or 1,2-di-substituted indan expressed by general formula (I’) wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, and X and OH group can be in either cis- or trans-configuration forming either a racemic body or an optically-active substance; or cis-1,2-epoxyindan expressed by general formula (VI) wherein R is phenyl or a lower alkyl group, oxazoline ring is in cis-configuration forming either a racemic body or an optically active substance is reacted, under an acidic condition, with a nitrile expressed by general formula (II) wherein R is phenyl or a lower alkyl group to produce cis-1-aminoindan-2-ol expressed by general formula (V) wherein NH2 and OH groups are in cis-configuration forming either a racemic body or an optically-active substance. STR1

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Extended knowledge of (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol

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alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases

The impact of moving the P1 side-chain from the beta-position to the alpha-position in norstatine-containing plasmepsin inhibitors was investigated, generating two new classes of tertiary alcohol-comprising alpha-benzylnorstatines and alpha-phenylnorstatines. Twelve alpha-substituted norstatines were designed, synthesized and evaluated for their inhibitory potencies against plasmepsin II and the plasmepsin IV orthologues (PM4) present in the digestive vacuole of all four Plasmodium species causing malaria in man. New synthetic routes were developed for producing the desired alpha-substituted norstatines as pure stereoisomers. The best compounds provided Ki values in the nanomolar range for all PM4, with a best value of 110 nM in PM4 from Plasmodium ovale. In addition, excellent selectivity over the closely related human aspartic protease Cathepsin D was achieved. The loss of affinity to Plasmodium falciparum PM4, which was experienced upon the move of the P1 substituent, was rationalized by the calculation of inhibitor-protein binding affinities using the linear interaction energy method (LIE).

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Discovery of 2,4-Dimethylpyridine

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Electric Literature of 108-47-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.108-47-4, Name is 2,4-Dimethylpyridine, molecular formula is C7H9N. In a Article£¬once mentioned of 108-47-4

Polyisobutylene-based miktoarm star polymers via a combination of?carbocationic and atom transfer radical polymerizations

Poly(isobutylene-b-styrene) (PIB-PS) copolymers and polyisobutylene (PIB) homopolymers were synthesized via quasiliving carbocationic polymerization from the initiator 3,3,5-trimethyl-5-chlorohexyl acetate, which contains a protected hydroxyl group. The PIB block was created at -70 C in a methylcyclohexane/methyl chloride (60:40) cosolvent system, using TiCl4 as co-initiator, followed optionally by sequential addition of styrene. Using a strong base, the acetate head group of the resulting block copolymer was cleaved to yield a hydroxyl group, which was subsequently esterified with the branching agent 2,2-bis((2-bromo-2-methyl)propionatomethyl)propionyl chloride (BPPC) to create dual initiating sites for atom transfer radical polymerization (ATRP). ATRP of tert-butyl acrylate was carried out using a Cu(I)Br/1,1,4,7,7-pentamethyldiethylenetriamine (PMDETA) catalyst system. In some cases, the ester side chains of the poly(tert-butyl acrylate) (PtBA) blocks were cleaved to create poly(acrylic acid) (PAA) blocks. The final miktoarm star polymers had compositions that were very close to theoretical.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Archives for Chemistry Experiments of (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol

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126456-43-7, Name is (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, belongs to chiral-nitrogen-ligands compound, is a common compound. SDS of cas: 126456-43-7In an article, once mentioned the new application about 126456-43-7.

Combinatorial library of indinavir analogues: Replacement for the aminoindanol at P2?

A 1X22X41 combinatorial library or 902 compounds of indinavir analogues was synthesized on the solid support to identify a replacement for the aminoindanol moiety at P2?. 2,6-Dimethyl-4-hydroxy phenol was discovered to be a good replacement for aminoindanol.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Extended knowledge of 108-47-4

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 108-47-4 is helpful to your research. Electric Literature of 108-47-4

Electric Literature of 108-47-4, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 108-47-4, molcular formula is C7H9N, introducing its new discovery.

Preparation of dithiophosphoric acid diester-halides

A process for the preparation of a dithiophosphoric acid diester-halide of the formula STR1 IN WHICH R1 is alkyl with 1 to 10 carbon atoms, aralkyl with 1 to 6 carbon atoms in the alkyl radical, or alkoxyalkyl or alkylthioalkyl with 1 to 5 carbon atoms in each alkyl radical, R2 is alkyl with 1 to 8 carbon atoms, and Hal is halogen, Which comprises reacting an S-alkyl or S-aralkyl ester of a dithiophosphoric acid dihalide of the formula STR2 WITH ABOUT A 5 TO 300% MOLAR EXCESS OF AN ALCOHOL OF THE FORMULA in the presence of about a 5 to 300% molar excess of a tertiary pyridine base or tertiary aralkyl-alkylamine at a temperature between about -10 and +60 C. Advantageously the tertiary base is pyridine, 2-, 3- or 4-methyl-pyridine, 4-ethyl-pyridine, 5-ethyl-2-methyl-pyridine, 2,4- or 2,6-dimethyl-pyridine, 2,4,6-trimethyl-pyridine, quinoline, isoquinoline, 2-, 4- or 6-methyl-quinoline, 6-chloro-2-methyl-quinoline, 2-chloro-4-methyl-quinoline, 8-chloro-2-methyl-quinoline or dimethylbenzylamine, the reaction is carried out at about 0 to 30 C., the alcohol is ethanol employed in about a 15 to 30% molar excess, about a 20 to 210% molar excess of the tertiary base is employed, R1 is alkyl with 1 to 8 carbon atoms, aralkyl with 1 to 3 carbon atoms in the alkyl radical, or alkoxyalkyl or alkylthioalkyl with 1 to 3 carbon atoms in each alkyl radical and Hal is chlorine.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

The important role of 2,4-Dimethylpyridine

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Product Details of 108-47-4, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 108-47-4, Name is 2,4-Dimethylpyridine, molecular formula is C7H9N

Pyridine: A Denaturant or Stabilizer of Spherical Nucleic Acids?

The spotlighted dual functions of pyridine as a denaturant and as a stabilizer for duplex DNA are thoroughly investigated using spherical nucleic acids (SNAs). At neutral pH, pyridine destabilizes the duplex interconnects of assembled SNAs, resulting in a gradual decrease in their melting temperature (Tm) as a function of the pyridine concentration. This result is in good agreement with the conventional role of pyridine as a powerful denaturant for free duplex DNA. On the contrary, the addition of pyridine dramatically increases the Tm of hybridized SNAs under acidic conditions, which could be a striking result of pyridine’s stabilizing effect for DNA duplex as previously suggested on the basis of the pyridine-nucleobase interactions. After comprehensive and quantitative investigation based on the analysis of the sharp melting transitions of SNAs, however, we report that, in fact, the pH increase induced by pyridine is also an essential parameter accounting for pyridine’s DNA-stabilizing effects under acidic conditions. Importantly, we prove that pyridine, particularly at a low concentration, does not increase the Tm of hybridized SNAs even under acidic conditions, if the pH increase by pyridine is corrected to maintain the same initial pH.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis