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Synthesis and cytotoxic evaluation of cis-locked and constrained analogues of combretastatin and combretastatin A4

A series of cis-locked stilbenic compounds related to combretastatin and combretastatin A4 has been designed and synthesized. The cytotoxic effects of these rigid analogues were evaluated as well as their abilities to inhibit tubulin polymerization.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H771NO – PubChem

 

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Discovery of N-Aroyl Diketone/Triketone Derivatives as Novel 4-Hydroxyphenylpyruvate Dioxygenase Inhibiting-Based Herbicides

4-Hydroxyphenylpyruvate dioxygenase (HPPD, EC 1.13.11.27) is an important target site for discovering new bleaching herbicides. To explore novel HPPD inhibitors with excellent herbicidal activity, a series of novel N-aroyl diketone/triketone derivatives were rationally designed by splicing active groups and bioisosterism. Bioassays revealed that most of these derivatives displayed preferable herbicidal activity against Echinochloa crus-galli (EC) at 0.045 mmol/m2 and Abutilon juncea (AJ) at 0.090 mmol/m2. In particular, compound I-f was more potent compared to the commercialized compound mesotrione. Molecular docking indicated that the corresponding active molecules of target compounds and mesotrione shared similar interplay with surrounding residues, which led to a perfect interaction with the active site of Arabidopsis thaliana HPPD.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H532NO – PubChem

 

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Design, synthesis and application of a new type of bifunctional Le-Phos in highly enantioselective gamma-addition reactions of N-centered nucleophiles to allenoates

A novel class of cyclic phosphine derived bifunctional catalysts (Le-Phos) is reported, which can be readily prepared from inexpensive and commercially available starting materials and exhibit good performances in enantioselective gamma-addition reactions of N-centered nucleophiles and allenoates under mild conditions. The salient features of this reaction include high product yields, good enantioselectivity, mild reaction conditions, and broad substrate scope and gram-scale scalability.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H919NO – PubChem

 

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Chemically modified mutant serine hydrolases show improved catalytic activity and chiral selectivity

This invention provides novel chemically modified mutant serine hydrolases that catalyze a transamidation and/or a transpeptidation and/or a transesterification reaction. The modified serine hydrolases have one or more amino acid residues in a subsite replaced with a cysteine, wherein the cysteine is modified by replacing the thiol hydrogen in the cysteine with a substituent group providing a thiol side chain comprising a moiety selected from the group consisting of a polar aromatic substituent, an alkyl amino group with a positive charge, and a glycoside. In particularly preferred embodiments, the substitutents include an oxazolidinone, a C1 to C15 alkyl amino group with a positive charge, or a glycoside.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H134NO – PubChem

 

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An improved procedure for the palladium-catalyzed oxidative carbonylation of beta-amino alcohols to oxazolidin-2-ones

A highly efficient oxidative cyclocarbonylation of beta-amino alcohols and 2-aminophenol to oxazolidin-2-ones has been achieved by using PdI2 in conjunction with KI as the catalytic system in DME under relatively mild conditions (100 C and 20 atm of a 4:1 mixture of CO and air).

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H540NO – PubChem

 

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Studies on a total synthesis of plakotenin: Synthesis of optically active trans-hydrindanes by diastereoselective asymmetric intramolecular diels-alder reaction

Diastereoselective asymmetric intramolecular Diels-Alder reaction of 5,5-(trimethylenedithio)-2(E),7(E),9-decatrienoyl amides (13a-e) having various chiral auxiliaries was performed to give optically active trans- hydrindanes, which would be an important intermediate for a total synthesis of plakotenin (1), was described. In the several chiral auxiliaries, Saigo’s oxazolidinone was found to give trans-hydrindane (15a) in the highest stereoselectivity (96% e.e.), after conversion to benzyl ester.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H644NO – PubChem

 

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Intermolecular and selective synthesis of 2,4,5-trisubstituted oxazoles by a gold-catalyzed formal [3+2] cycloaddition

Oxazole new world: A gold-catalyzed intermolecular reaction of pyridine-N-aminides with ynamides can be used to prepare trisubstituted 1,3-oxazoles with a variety of functional groups. This formal [3+2] cycloaddition employs robust conjugated N-ylides as N-nucleophilic N-acyl nitrene equivalents for a highly chemoselective and regioselective addition across electron-rich C-C triple bonds.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H473NO – PubChem

 

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Kinetic resolution of racemic carboxylic acids by an L-histidine-derived sulfonamide-induced enantioselective esterification reaction

(Chemical Equation Presented) The direct and catalytic kinetic resolution of racemic carboxylic acids bearing a Bronsted base such as O-protected alpha-hydroxy carboxylic acids and N-protected alpha-amino acids has been accomplished through an L-histidine-derived sulfonamide-induced enantioselective esterification reaction with tert-butyl alcohol for the first time. Highly asymmetric induction [S(kfast/kslow) = up to 56] has been achieved under the equilibrium between a chiral catalyst and two diastereomeric acylammonium salts through an intramolecular hydrogen-bonding interaction.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H641NO – PubChem

 

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BENZAMIDE CGRP RECEPTOR ANTAGONISTS

The present invention is directed to benzamide compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H71NO – PubChem

 

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PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This document discloses molecules having the following formula (?Formula One?): and processes related thereto.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H42NO – PubChem