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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

 

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Herbicidal acetamides

Herbicidal bromo- or chloroacetamides of the formula: STR1 where R is alkyl or alkoxy of 1 to 4 carbon atoms; R1 is hydrogen or alkyl of 1 to 3 carbon atoms; R2 is hydrogen or methyl; R3 is hydrogen or methyl; X is chlorine or bromine; and Y is oxygen or sulfur.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H62NO – PubChem

 

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A research for some oxazolidinones to evaluate their antimicrobial activity

Objectives: In this research, antimicrobial activity of some new oxazolidinone derivatives were evaluated against S. aureus ATCC 25923, E. coli ATCC 25922, B. subtilis ATCC 6633, methicillin-resistant Staphylococcus aureus (MRSA) clinical isolate and C. albicans ATCC 10231. Material and Method: Formerly obtained and published 10 oxazolidinones were tested against antimicrobial activity and this evaluation was carried out in Mueller-Hinton broth and Sabouraud dextrose broth. Result and Discussion: Compounds E5, and E9 showed antimicrobial activity against both bacteria and fungi with 25 mug/mL and 50 mug/mL, respectively. Our present research and the others have shown that the electro-negativity degree is very important for the biological activity.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H715NO – PubChem

 

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SULFONAMIDE COMPOUNDS AS VOLTAGE-GATED SODIUM CHANNEL MODULATORS

The present invention relates to sulfonamide compounds Formula (I) wherein the substituents are as described herein, and their use in a medicine for the treatment of diseases, disorders associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. It further relates to the compounds herein and their pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof useful in treating diseases, disorders, syndromes and/or conditions associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. The invention also relates to process for the preparation of the compounds of the invention. (I)

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Oxazolidine – Wikipedia,
Oxazolidine | C3H207NO – PubChem

 

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VINYL FLUORIDE CYCLOPROPYL FUSED THIAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE

The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A7, and each of Ra, Rb, R1, R2, R3, R8 R9 and R10 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Abeta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer’s Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H11NO – PubChem