Category: 144542-43-8

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From amino acids to fused chiral pyrrolidines and piperidines via the INOC route

Intramolecular nitrile oxide olefin cycloaddition (INOC) reactions of oximes 1-3 and of 24-27 derived from 1-amino acids have been found to proceed stereoselectively, yielding tricyclic fused pyrrolidines and piperidines. Further manipulation led to chiral hydroxymethyl-substituted fused piperidines 33-35 and to 3-amino-4-(1-hydroxypropyl)-2-mercaptomethyl-N- methylpiperidine (36). The structures and stereochemistries of the fused systems, as well as those of the piperidines, have been established by NMR.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Formula: C5H7NO4, you can also check out more blogs about144542-43-8

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Oxazolidine | C3H1468NO – PubChem

 

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Utilization of L-serine in an oxime olefin cycloaddition route to a functionalized asymmetric pyrrolidine, a selective alpha-glucosidase inhibitor

A new route for asymmetric aza-sugar analogs starting with L-serine and utilizing an intramolecular oxime olefin cycloaddition has been successfully developed. A member of this family of branched chain sugar amino di(hydroxymethyl) pyrrolidines (1 and 2) exhibits selective inhibition of alpha-glucosidase, while no inhibition of beta-glucosidase was detected.

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DERIVATIVES OF 2-AMINO-4-(2-OXAZOLIDINON-3-YL)-PYRIMIDINE FUSED WITH A FIVE-MEMBERED HETEROAROMATIC RING IN 5,6-POSITION WHICH ARE USEFUL FOR THE TREATMENT OF VARIOUS CANCERS

The present invention relates to compounds of general Formula (I), uses of the compound of general Formula (I) for use in the treatment or prophylaxis of a disorder of the human or animal body, and pharmaceutical compositions comprising a therapeutically effective amount of the compounds of general Formula (I) as active ingredients.

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 144542-43-8 is helpful to your research. Reference of 144542-43-8

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Oxazolidine | C3H1458NO – PubChem

 

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IOOC route to substituted chiral pyrrolidines. Potential glycosidase inhibitors

Branched-chain five-membered ring aza-sugar analogues, synthesized from amino acids by an intramolecular oxime-olefin cycloaddition reaction, the IOOC route, were found to be selective glycosidase inhibitors. The derivative 2,4(S)-di(hydroxymethyl)-3(S)-aminopyrrolidine, obtained from D-serine, was about 1 order of potency more active than its enantiomer obtained from L- serine.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1467NO – PubChem

 

Electric Literature of 144542-43-8, 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, 144542-43-8, molcular formula is C5H7NO4, introducing its new discovery.

Synthesis of tryptophans by Lewis acid promoted ring-opening of aziridine-2-carboxylates: Optimization of protecting group and Lewis acid

The preparation of tryptophan derivatives through the Lewis acid promoted substitution of aziridine carboxylates with indole was found to be accompanied by a ring-expansion reaction to generate an oxazolidinone byproduct. The ratio of tryptophan to oxazolidinone products can be optimized through a judicious choice of Lewis acid and N-protecting group.

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Fluorogenic peptide substrates for serine and threonine phosphatases

Figure presented A new fluorescent assay for Ser/Thr protein phosphatases has been developed. Hydrolysis of a phosphoSer residue liberates the Ser hydroxyl group, which induces a cyclization reaction on the N-terminal carbamate and releases a fluorescent reporter. Sequence selectivity is observed using several peptide substrates against alkaline phosphatase (ALP), bacteriophage protein phosphatase (-PPase), and vaccinia H1 related phosphatase (VHR). These studies suggest that the assay could be a useful tool for profiling the substrate specificities of medicinally important phosphatases.

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Oxazolidine | C3H1485NO – PubChem

 

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Synthesis and biological activity of S-oxo-[(methylthio)-methyl]cysteinols

A convenient route was developed to synthesize S-oxo-[(methylthio)-methyl]cysteinols on a large scale from cheap l-serine as the starting material. The structures of diastereoisomers were determined by NMR, CD spectra, and X-ray diffraction analysis. All four diastereoisomers were examined for their ability to inhibit certain bacteria from growing.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 144542-43-8

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1483NO – PubChem

 

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, HPLC of Formula: C5H7NO4, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 144542-43-8, Name is (R)-Methyl 2-oxooxazolidine-4-carboxylate, molecular formula is C5H7NO4

NOVEL BENZODIOXANE-PIPERIDINE DERIVATIVES AND THEIR THERAPEUTIC APPLICATIONS FOR TREATING NEUROPSYCHIATRIC DISORDERS

The present invention concerns benzodioxane-piperidine with general formula I: wherein notably: R1 represents one or more identical or different substituent(s) on the benzene ring, each independently representing a hydrogen or halogen atom, or a C1-4 alkyl group, or a C1-4 alkoxy group or a C1-4 hydroxyalkyl group or a C1-4 alkylcarbonyl or an alkoxycarbonyl group or an OH group or an SO2R group with R alkyl, or a CN group, or a CF3 group, or an OCF 3 group; n=1, 2 or 3; m=0 or 1, and R2 represents one or more identical or different substituent(s) on the oxazolidinone or morpholinone ring, each independently representing: a hydrogen atom, a C1-4 alkyl group, or a C1-4 alkoxy group, or a C1-4 hydroxyalkyl group, or an alkylcarbonyl group, or an alkoxycarbonyl group, or an alkoxyphenyl group.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. HPLC of Formula: C5H7NO4, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 144542-43-8, in my other articles.

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A New Electrophilic Alaninol Synthon. A General Route to Oxazolidinones of D or (R)-2-Amino Alcohols from L-Serine

A new electrophilic alaninol synthon, (S)-4-(4′-tolylsulfonyloxymethyl)oxazolidin-2-one, derived from serine, undergoes nucleophilic displacements with Gilman cuprates and/or Grignard/CuX reagents in high yields to provide (R)-4-substituted oxazolidinones.

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Enhanced enantiocontrol in catalytic metal carbene transformations with dirhodium(II) tetrakis, Rh2(4S-MEOX)4

The synthesis, spectral characteristics, and X-ray structures for dirhodium(II) tetrakis, Rh2(4S-MEOX)4, and the related dirhodium(II) tetrakis, Rh2(4S-THREOX)4, are reported.Comparison is made between these 2-oxooxazolidin-ligated dirhodium(II) catalysts for metal carbene transformations and those with comparable 2-oxopyrrolidine ligands, especially dirhodium(II) tetrakis, Rh2(5S-MEPY)4.Structure-selectivity comparisons reveal that Rh2(4S-MEOX)4 provides higher enantiocontrol and, in some cases, higher diastereocontrol than Rh2(5S-MEPY)4 in intramolecular carbon-hydrogen insertion reactions of sterically demanding diazoacetates and diazoacetamides and is the catalyst of choice for highly enantioselective diazodecomposition of adamantyl diazoacetates and N-(tert)butyldiazoacetamides.The structurally analogous Rh2(4S-THREOX)4 is nearly identical with Rh2(4S-MEOX)4 in its overall effect on selectivity.The net advantage of Rh2(4S-MEOX)4 lies in its wider openness for metal carbene transformations.

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