Heterocyclic Building Blocks-Oxazolidine

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: 22625-57-6, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 22625-57-6, name is 5-(Chloromethyl)oxazolidin-2-one. In an article£¬Which mentioned a new discovery about 22625-57-6

Quinoline-aminomethyl-pyridyl derivatives with anti-helicobacter activity

Compounds of formula (I) in which the substituents and symbols have the meanings indicated in the description, are suitable for the control of Helicobacter bacteria.

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Synthesis, spectroscopic characterization, and in vitro antibacterial evaluation of novel functionalized sulfamidocarbonyloxyphosphonates

Several new sulfamidocarbonyloxyphosphonates were prepared in two steps, namely carbamoylation and sulfamoylation, by using chlorosulfonyl isocyanate (CSI), alpha-hydroxyphosphonates, and various amino derivatives and related (primary or secondary amines, beta-amino esters, and oxazolidin-2-ones). All structures were confirmed by 1H, 13C, and 31P NMR spectroscopy, IR spectroscopy, and mass spectroscopy, as well as elemental analysis. Eight compounds were evaluated for their in vitro antibacterial activity against four reference bacteria including Gram-positive Staphylococcus aureus (ATCC 25923), and Gram-negative Escherichia coli (ATCC 25922), Klebsiella pneumonia (ATCC 700603), Pseudomonas aeruginosa (ATCC 27853), in addition to three clinical strains of each studied bacterial species. Compounds 1a?7a and 1b showed significant antibacterial activity compared to sulfamethoxazole/trimethoprim, the reference drug used in this study.

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“Click” synthesis of small molecule probes for activity-based fingerprinting of matrix metalloproteases

By using “Click Chemistry”, we achieved the facile synthesis of various affinity-based hydroxamate probes that enable generation of activity-based fingerprints of a variety of metalloproteases, including matrix metalloproteases (MMPs), in proteomics experiments. The Royal Society of Chemistry 2006.

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Imidazolium and Potassium Hydrogen Carbonate Salts as Ecofriendly Organocatalysts for Oxazolidinone Synthesis

Although oxazolidinones are valuable intermediate compounds for industrial applications, no synthetic method is suitable for their production on a large scale owing to the use of reagents/catalysts that are hazardous or toxic to human health or ecotoxic for the environment. In this manuscript, we describe new and efficient catalysts, that is, the nontoxic hydrogen carbonate anion in combination with a potassium or diisobutylimidazolium ([iBu2IM]) countercation, for the conversion of beta-amino alcohols into cyclic oxazolidinones in high yields of 69 to 90 %. Depending on the catalytic conditions, both catalysts could be easily recovered from the crude reaction products and reused several times without a decrease in their catalytic performance. Furthermore, the imidazolium cation is a renewable catalyst, because its preparation requires less than 10 % of carbon fossil sources.

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of (R)-4-Benzyl-2-oxazolidinone, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 102029-44-7, Name is (R)-4-Benzyl-2-oxazolidinone, molecular formula is C10H11NO2

NOVEL MACROCYCLES AS FACTOR XIA INHIBITORS

The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

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Application of 16251-45-9, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.16251-45-9, Name is (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one, molecular formula is C10H11NO2. In a article£¬once mentioned of 16251-45-9

Heteroaromatic side-chain analogs of pregabalin

A series of heteroaromatic analogs of pregabalin has been identified that possess anticonvulsant activity in the DBA/2 mouse model. The methods of synthesis and preliminary pharmacology are discussed herein.

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Electric Literature of 102029-44-7, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 102029-44-7, Name is (R)-4-Benzyl-2-oxazolidinone,introducing its new discovery.

BIPHENYL CARBOXYLIC ACIDS AND DERIVATIVES THEREOF

The present invention relates to compounds having the general Formula (I) with the definitions of R1, R2, R3, and R4 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer”s disease and their use for the modulation of gamma-secretase activity.

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A medicine intermediate N – Boc – trans -4 – methyl – L – proline methyl ester preparation method (by machine translation)

The invention discloses a N – Boc – trans – 4 – methyl – L – proline methyl ester preparation method, compound D – glutamic acid in the diazotization reaction, esterification reaction, hydrolysis to obtain compound 16; compound 16 with TBSCl reaction to obtain compound 17; compound 17 hydrolysis, then with the (R)- 4 – benzyl – 2 – oxazolidinone reaction to obtain compound 18; compound 18 undergo the substitution reaction to obtain compound 19; compound 19 reduction to obtain compound 20, then with the DPPA, DBU reaction, to obtain the compound 21; compound 21 deprotection to obtain compound 22; compound 22 dehydroxylated, and then dissolved in methanol in the reaction under the condition of iodine potassium hydroxide to obtain compound 23; compound 23 deprotected after reaction with P-toluene sulfonyl chloride, to obtain compound 24; compound 24 in the catalytic reaction under the condition of the ring, adding alkaline substance and Boc anhydride reaction to obtain compound 4. Preparation method of the invention overcomes the existing technology in the preparation N – Boc – 4 – methyl proline methyl ester exists when the defect of the stereo selectivity is not good, the use of a readily available and inexpensive starting materials, to improve the yield of the process. (by machine translation)

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Design and synthesis of highly potent benzodiazepine gamma-secretase inhibitors: Preparation of (2S,3R)-3-(3,4- difluorophenyl)-2-(4-fluorophenyl)-4-hydroxy-N-((3S)-1-methyl-2-oxo-5- phenyl-2,3-dihydro-1H-benzo[e][1,4]-diazepin-3-yl)butyramide by use of an asymmetric Ireland-Claisen rearrangement

Novel benzodiazepine-containing gamma-secretase inhibitors for potential use in Alzheimer’s disease have been designed that incorporate a substituted hydrocinnamide C-3 side chain. A syn combination of alpha-alkyl or aryl and beta-hydroxy or hydroxymethyl substituents was shown to give highly potent compounds. In particular, (2S,3R)-3-(3,4-difluorophenyl)-2-(4-fluorophenyl)-4-hydroxy- N-((3S)-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)butyramide (34) demonstrated excellent in vitro potency (IC50 = 0.06nM). 34 could also be selectively methylated to give [3H]-28, which is of use in radioligand binding assays.

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95715-86-9, Name is Methyl (R)-N-Boc-2,2-dimethyloxazolidine-4-carboxylate, belongs to oxazolidine compound, is a common compound. Safety of Methyl (R)-N-Boc-2,2-dimethyloxazolidine-4-carboxylateIn an article, once mentioned the new application about 95715-86-9.

2-Thiazolyl alpha-amino ketones: A new class of reactive intermediates for the stereocontrolled synthesis of unusual amino acids

The thiazole-based one carbon homologation of four alpha-amino acids (L-phenylalanine, L-leucine, L-threonine, and L-serine) to the corresponding alpha-hydroxy beta-amino aldehydes and acids in both configurations at C(alpha), is described. The methodology involves the following key operations: (i) the conversion of an alpha-amino ester to a 2-thiazolyl alpha-amino ketone; (ii) the stereocontrolled reduction of a ketone carbonyl to either syn or anti alpha,beta-amino alcohols; (iii) the aldehyde release from the thiazole ring; (iv) the oxidation of the aldehyde to a carboxylic acid. The methodology was only partially applied to L-phenylglycine because of some limitations in operation (i).

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