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Conjugate addition of aryl nucleophiles to alpha,beta-unsaturated cinnamic acid derivatives containing Evans type chiral auxiliaries

Cinnamides containing oxazolidin-2-one type auxiliaries have been prepared. A novel pathway to chiral 4-aryl-6-methyl-3,4-dihydrocoumrines via the asymmetric conjugate addition of arylmagnesium bromides to these cinnamides is described.

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Oxazolidine – Wikipedia,
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Copper-mediated amidation of heterocyclic and aromatic C-H bonds

A copper-mediated aerobic coupling reaction enables direct amidation of heterocycles or aromatics having weakly acidic C-H bonds with a variety of nitrogen nucleophiles. These reactions provide efficient access to many biologically important skeletons, including ones with the potential to serve as inhibitors of HMTs.

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Electric Literature of 695-53-4, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 695-53-4, 5,5-Dimethyloxazolidine-2,4-dione, introducing its new discovery.

Inter-laboratory assessment of a harmonized zebrafish developmental toxicology assay – Progress report on phase I

This report provides a progress update of a consortium effort to develop a harmonized zebrafish developmental toxicity assay. Twenty non-proprietary compounds (10 animal teratogens and 10 animal non-teratogens) were evaluated blinded in 4 laboratories. Zebrafish embryos from pond-derived and cultivated strain wild types were exposed to the test compounds for 5 days and subsequently evaluated for lethality and morphological changes. Each of the testing laboratories achieved similar overall concordance to the animal data (60-70%). Subsequent optimization procedures to improve the overall concordance focused on compound formulation and test concentration adjustments, chorion permeation and number of replicates. These optimized procedures were integrated into a revised protocol and all compounds were retested in one lab using embryos from pond-derived zebrafish and achieved 85% total concordance. To further assess assay performance, a study of additional compounds is currently in progress at two laboratories using embryos from pond-derived and cultivated-strain wild type zebrafish.

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Oxazolidine – Wikipedia,
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Direct intramolecular catalytic enantioselective alkylation of oxazolidinone bromoalkanoate imides

Bromoalkanoate imides undergo intramolecular alkylation to form cyclopentane carboximides using catalytic amounts of magnesium bromide in the presence of DBU. Addition of PyBox ligands affords alkylation products with moderate enantioselectivity.

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Oxazolidine – Wikipedia,
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Regioselective Rh(I)-catalyzed sequential hydrosilylation toward the assembly of silicon-based peptidomimetic analogues

A highly regioselective Rh(I)-catalyzed hydrosilylation of enamides is presented. This mild protocol allows access to a wide variety of different arylsilanes with substitution at the beta-position of the enamide and functionalization on the alkyl chain tethered to the silane. This protocol is extended to include a sequential one-pot hydrosilylation. Using diphenylsilane as the appendage point, hydrosilylation of a protected allyl alcohol followed by hydrosilylation of an enamide generates a complex organosilane in one step. This highly convergent strategy to synthesize these functionalized systems now provides a way for the rapid assembly of a diverse collection of silane-based peptidomimetic analogues.

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Oxazolidine – Wikipedia,
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5-ALKYLTHIO-7-[(4-ARYLBENZYL)AMINO]-1(2)H-PYRAZOLO[4,3-D]PYRIMIDINES FOR TREATMENT OF LYMPHOMA

The present invention relates to 5-alkylthio-7-[(4-arylbenzyl)amino]-1(2)H-pyrazolo[4,3-d]pyrimidine derivatives of formula I which are effective inhibitors of kinases and exhibit strong antiproliferative and proapoptotic properties on lymphoma cells. This invention further relates to use of said derivatives in the treatment of blood hyperproliferative diseases, such as Non-Hodgkin lymphomas.

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Oxazolidine – Wikipedia,
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Intermediates and processes for preparing substituted chromanol derivatives

The invention relates to processes for preparing a compound of the formula 1 and the enantiomer of said compound, wherein the benzoic acid moiety is attached at position 6 or 7 of the chroman ring, and R1, R2, and R3 are as defined herein. The invention further relates to intermediates that are useful in the preparation of the compound of formula X above.

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Oxazolidine – Wikipedia,
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Effects of novel polyhedral oligomeric silsesquioxane containing hydroxyl group and epoxy group on the dicyclopentadiene bisphenol dicyanate ester composites

Two types of novel Polyhedral Oligomeric Silsesquioxanes respectively containing hydroxyl group and epoxy group (P-POSS and E-POSS) were achieved and evaluated. The structure had been characterized by IR spectra and NMR spectra. Dicyclopentadiene bisphenol dicyanate ester (DCPDCE) composites were then prepared using P-POSS and E-POSS respectively. Their effect on the curing kinetics, dielectric, mechanical, flame-retardant and thermal properties and water absorption of the resulting composites were investigated. The results suggested that the addition of modified POSS could facilitate the curing reaction of DCPDCE. Besides, the DCPDCE composites containing modified POSS exhibited excellent flame-retardant property over pure DCPDCE resin. Adding only a little amount as small as 1.5?wt% P-POSS or 2.5?wt% E-POSS could change the UL-94V of DCPDCE resin from V-2 to V-0. The composite with P-POSS exhibited better flame-retardant and thermal properties than the composite with E-POSS. However, composite filled with E-POSS presented better dielectric property and lower water absorption.

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Oxazolidine – Wikipedia,
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3-Aryl-2-oxazolidinones through the palladium-catalyzed N-arylation of 2-oxazolidinones.

[reaction: see text] 3-Aryl-2-oxazolidinones are obtained in good yields through the palladium-catalyzed N-arylation of 2-oxazolidinones with aryl bromides. The nature of aryl bromides, phosphine ligands, bases, and solvents strongly affects the reaction outcome.

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STEREOCHEMISTRY OF RINGS. XV. gamma-LACTONE DERIVATIVES. Part 9. X-ray structure of 5-chloromethyl-2-oxazolidinone

C4H6NO2Cl (Mr=135.55) crystallizes in the monoclinic system, space group P21/c with a=9.257(2), b=5.181(3), c=12.620(2) Angstroem, beta=110.75(4) deg, V=566.0(4) Angstroem3, Z=4, Dc=1.59 g cm-1, mu(CuKalpha)=53.16 cm-1, lambda/=1.5418 Angstroem, F(000)=280.The oxazolidinone ring is approximately planar; the geometrical parameters reveal a certain degree of electronic delocalization in the molecule.The CH2Cl group assumes an axial position.The molecules are joined in dimers by strong N-H…O hydrogen bonds.

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