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Enantioselective Construction of Acyclic Quaternary Carbon Stereocenters: Palladium-Catalyzed Decarboxylative Allylic Alkylation of Fully Substituted Amide Enolates

We report a divergent and modular protocol for the preparation of acyclic molecular frameworks containing newly created quaternary carbon stereocenters. Central to this approach is a sequence composed of a (1) regioselective and -retentive preparation of allyloxycarbonyl-trapped fully substituted stereodefined amide enolates and of a (2) enantioselective palladium-catalyzed decarboxylative allylic alkylation reaction using a novel bisphosphine ligand.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1021NO – PubChem

 

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Single heterocyclic compounds as monoamine oxidase inhibitors: From past to present

Inhibitors of monoamine oxidase (MAO) have shown therapeutic values in a variety of neu-rodegenerative diseases such as depression, Parkinson?s disease and Alzheimer?s disease. Heterocyclic compounds exhibit a broad spectrum of biological activities and vital leading compounds for the development of chemical drugs. Herein, we focus on the synthesis and screening of novel single hetero-cyclic derivatives with MAO inhibitory activities during the past decade. This review covers recent pharmacological advancements of single heterocyclic moiety along with structure-activity relationship to provide better correlation among different structures and their receptor interactions.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H1254NO – PubChem

 

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METHOD FOR THE PRODUCTION OF THERMOPLASTIC POLYOXAZOLIDINONE POLYMERS

A process for producing thermoplastic polyoxazolidinone, comprising the following steps: (i) Reaction of a diisocyanate compound (A) with a bisepoxide compound (B) in the presence of a catalyst (C) and a compound (D) in a solvent (E) forming an intermediate compound (F) and (ii) Reaction of a compound (G) with the intermediate (F) formed in step (i), wherein compound (D) is one or more compounds selected from the group consisting of monofunctional isocyanate and monofunctional epoxide, and wherein compound (G) is an alkylene oxide. The invention is also related to the resulting thermoplastic polyoxazolidinone.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H237NO – PubChem

 

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Exposure to pesticides and mental disorders in a rural population of Southern Brazil

Introduction Exposure to pesticides has been associated with mental disorders, especially in occupationally exposed populations, such as farmers. This effect has been attributed to the neurotoxic and endocrine-disrupting activity of pesticides, as suggested by experimental studies. Objective To determine the prevalence of common mental disorders and self-reported depression, and analyze their association with the exposure to pesticides in a rural population resident in the municipality of Dom Feliciano, Rio Grande do Sul, where tobacco farming is the main economic activity. Methodology A cross-sectional study evaluating the prevalence of common mental disorders and self-reported depression in a sample of 869 adult individuals resident in Dom Feliciano, between October 2011 and March 2012 was performed. The evaluation of common mental disorders was performed using the Self-Reporting Questionnaire (SRQ-20), setting a cutoff point of 8 for both genders. A standardized questionnaire was used to obtain information on self-reported depression upon prior diagnosis by a health professional, and self-reported exposure to pesticide. In order to evaluate the association between exposure to pesticides and mental disorders, a non-conditional multivariate logistic regression analysis was performed. Results The prevalence of common mental disorders and self-reported depression in the sample population were 23% and 21%, respectively. Among individuals who reported depression, an increase of 73% was observed in the odds of pesticide exposure at an age equal to or less than 15 years. There was a positive association between self-reported pesticide poisoning and common mental disorders (OR?=?2.63; 95% CI, 1.62-4.25) as well as self-reported depression (OR?=?2.62; 95% CI, 1.63?4.21). Individuals who reported depression had a greater odds of exposure to pyrethroids (OR?=?1.80; 95% CI, 1.01?3.21) and aliphatic alcohol (OR?=?1.99; 95% CI, 1.04?3.83). An SRQ?20???8 was associated with an approximately seven times higher odds of exposure to aliphatic alcohol (95% CI, 1.73?27.53). Self-reported depression positively correlated with a greater period of exposure to dinitroaniline (OR?=?2.20; 95% CI, 1.03?4.70) and sulphonylurea (OR?=?4.95; 95% CI, 1.06?23.04). Conclusion The results suggest that exposure to pesticides could be related mental disorders. However, other common risk factors in tobacco farming, the main local economic activity, cannot be excluded.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1228NO – PubChem

 

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Copper-promoted iodovinylation of amides: synthesis of beta-functionalized enamides

We studied the addition of nitrogen radicals to ynol ethers in order to form beta-functionalized enamides. Poor yields are reported. On the other hand, we observed that copper coupling between 1,2-diiodoethene and various amides leads to beta-functionalized enamides in high yields with complete stereocontrol.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H951NO – PubChem

 

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Highly Selective Syn Addition of 1,3-Diones to Internal Ynamides Catalyzed by Zinc Iodide

1,3-Diones are already established as nucleophiles to perform additions to ynamides; the highly selective hydroalkoxylation of internal ynamides is now described. Several catalytic systems have been compared to perform this transformation, including transition-metal-based catalysts and Lewis acids. ZnI2 was found to be both very active and highly selective providing only E adducts through a syn addition. Investigation of the scope and limitations showed that this catalyst was compatible with various functional groups. In addition to seventeen examples of ynamide hydroalkoxylation, one example of ynamide hydroarylation is reported.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H904NO – PubChem

 

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Extensive dataset for oxidative degradation of ethanolamine at 55-75 c and oxygen concentrations from 6 to 98%

Post combustion CO2 capture using amines as chemical absorbents is a relatively mature technology. Rate of reaction and desorption energy demand are normally prime criteria for evaluation of new solvents while degradation and corrosion studies are often postponed. However, degradation and corrosion are in many cases showstoppers and should be considered at an early stage. In this work, a systematic study has been conducted on oxidative degradation of 30 wt% ethanolamine (MEA) for oxygen concentrations: 6, 21, 49 and 98% and temperatures: 55, 65 and 75 C. The formation of ten primary degradation compounds (acids, ammonia and alkyl amines) and seven secondary degradation compounds (HEGly, OZD, HEPO, HEF, HEA, HEI and BHEOX was monitored as function of time over a period of 3-6 weeks. The full comprehensive data set is available in the supplementary information for development of models describing the degradation behavior. Suggested mechanisms for formation of seven secondary degradation compounds; HEGly, HEPO, OZD, HEF, HEA, BHEOX and HEI from literature were compiled and discussed in view of the experimental results to suggest pathways which are more likely than others. The rate of MEA degradation increases with increasing temperature and oxygen concentration. The overall nitrogen balances were closed within 83-97%; the higher deviations observed at the highest temperature, 75 C. HEF, HEI and ammonia were the degradation compounds that most significantly contributed to the nitrogen balance in most experiments. However, at 6% O2 content, HEGly was the major nitrogen containing degradation compound identified. Formate was found to be the major anionic compound in all experiments. HEGly formation was found to be independent on O2 partial pressure, but this may not be true for the further reaction of HEGly. The results suggests OZD formation to be oxygen dependent. However, only one mechanism is so far suggested for an oxygen dependent pathway. Both OZD and HEPO concentrations increase with oxygen concentration. Separate laboratory experiments at constant temperature (55-75 C) do not capture the HEPO formation seen in pilot plant samples indicating that higher temperatures and/or temperature cycles are necessary. The results clearly show that performing accelerated degradation tests with 98% oxygen cannot easily be extrapolated to what happens at 6% oxygen, and therefore may not be representative for the situation in an industrial plant both with regard to rates of formation and products formed.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1097NO – PubChem

 

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INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras

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Oxazolidine – Wikipedia,
Oxazolidine | C3H79NO – PubChem

 

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A straightforward enantioselective synthesis of F17807

An efficient approach for the enantioselective synthesis of the 1,4-benzodioxane F17807 drug is reported. The developed route relied on two key steps, namely SNAr and Mitsunobu reactions, which permitted a straightforward access to the title compound with full preservation of the enantiomeric excess throughout the synthetic sequence.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H289NO – PubChem

 

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IMIDAZOPYRIMIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER

A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R3, R4, R6, and R7 are as defined herein.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H49NO – PubChem