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Improved synthesis of chiral N-protected allylic amines

The alpha-ester group of N-protected alpha-amino esters was reduced with diisobutylaluminum hydride to an intermediate aluminoxy acetal that on reaction with a Wittig reagent afforded the title chiral compounds in 48-78% chemical yields.

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Oxazolidine – Wikipedia,
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Electric Literature of 95715-86-9, 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, 95715-86-9, molcular formula is C12H21NO5, introducing its new discovery.

3-Ketone-4,6-diene ceramide analogs exclusively induce apoptosis in chemo-resistant cancer cells

Multidrug-resistance is a major cause of cancer chemotherapy failure in clinical treatment. Evidence shows that multidrug-resistant cancer cells are as sensitive as corresponding regular cancer cells under the exposure to anticancer ceramide analogs. In this work we designed five new ceramide analogs with different backbones, in order to test the hypothesis that extending the conjugated system in ceramide analogs would lead to an increase of their anticancer activity and selectivity towards resistant cancer cells. The analogs with the 3-ketone-4,6-diene backbone show the highest apoptosis-inducing efficacy. The most potent compound, analog 406, possesses higher pro-apoptotic activity in chemo-resistant cell lines MCF-7TN-R and NCI/ADR-RES than the corresponding chemo-sensitive cell lines MCF-7 and OVCAR-8, respectively. However, this compound shows the same potency in inhibiting the growth of another pair of chemo-sensitive and chemo-resistant cancer cells, MCF-7 and MCF-7/Dox. Mechanism investigations indicate that analog 406 can induce apoptosis in chemo-resistant cancer cells through the mitochondrial pathway. Cellular glucosylceramide synthase assay shows that analog 406 does not interrupt glucosylceramide synthase in chemo-resistant cancer cell NCI/ADR-RES. These findings suggest that due to certain intrinsic properties, ceramide analogs’ pro-apoptotic activity is not disrupted by the normal drug-resistance mechanisms, leading to their potential use for overcoming cancer multidrug-resistance.

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As cell necrosis inhibitors of the indole compounds (by machine translation)

The invention relates to chemical formula (1) indole compounds, or its pharmaceutically acceptable salt or isomer, and in containing the same as the characteristic, as an active ingredient for the prevention or treatment of cell necrosis and its associated disease composition and method of manufacturing. (by machine translation)

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Tunable Stereoselectivity in the Addition of 2-Lithiothiazole to L-Serinal Derived N-Benzyl Nitrone. Synthesis of C-2 Epimer 2,3-Diamino-4-Hydroxybutanals

A complete reversal of diastereoselectivity (ds <*> 95percent) in the addition of 2-lithiothiazole to L-serinal derived N-benzyl nitrone has been achieved by the change of the hydroxy and amino protective groups in the aldehyde moiety; the resultant epimeric 2-thiazolyl N-benzyl hydroxylamines were converted to C-2 epimer 2,3-diamino-4-hydroxybutanals via reductive dehydroxylation and thiazolyl-to-formyl conversion.

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Oxazolidine – Wikipedia,
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Synthesis of 2-amino-octa-4,7-dien-1-ol (2): Key intermediate for mycothiazole natural product and analogs

Starting from L-aminoacids, facile methods for the preparation 2-aminocta-4,7-dien-ol with different stereochemistry have been developed as key intermediates of mycothiazole and analogs. Copyright Taylor & Francis, Inc.

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Oxazolidine – Wikipedia,
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An efficient one-pot oxidative esterification of aldehydes to carboxylic esters using B(C6F5)3-TBHP

A simple and efficient protocol for oxidative esterification of diverse aldehydes with alcohols was accomplished with tert-butyl hydroperoxide and 1 mol % of tris(pentafluorophenyl)borane [B(C6F5)3] to generate the corresponding esters in good to excellent yields. The present protocol represents compatibility with wide range of functional groups as well as exceptional tolerance toward acid labile protecting groups such as TBDPS, TBDMS, acetonide, and Boc.

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INDOLE COMPOUND AS INHIBITOR OF NECROSIS

The present invention relates to an indole compound represented by formula (1), a pharmaceutically acceptable salt or isomer thereof, a composition for prevention or treatment of necrosis and necrosis-associated diseases, and a method for preparing the composition, the composition comprising the indole compound or the pharmaceutically acceptable salt or isomer thereof as an active ingredient.

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Complete structure elucidation of shishididemniols, complex lipids with tyramine-derived tether and two serinol units, from a marine tunicate of the family Didemnidae

(Chemical Equation Presented) Two new serinolipid derivatives, shishididemniols A (1) and B (2), were isolated as antibacterial constituents of a tunicate of the family Didemnidae. The structure of 1 was elucidated by interpretation of spectral data and the application of the modified Mosher method to 1 and its suitable degradation products. Compound 2 was the chlorohydrin of 1. Compounds 1 and 2 exhibited antibacterial activity against fish pathogenic bacterium Vibrio anguillarum.

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Modular Synthesis of Diverse Natural Product-Like Macrocycles: Discovery of Hits with Antimycobacterial Activity

A modular synthetic approach was developed in which variation of the triplets of building blocks used enabled systematic variation of the macrocyclic scaffolds prepared. The approach was demonstrated in the synthesis of 17 diverse natural product-like macrocyclic scaffolds of varied (12?20-membered) ring size. The biological relevance of the chemical space explored was demonstrated through the discovery of a series of macrocycles with significant antimycobacterial activity.

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Hepatitis C Virus Inhibitors

The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.

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Oxazolidine – Wikipedia,
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