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The present invention is directed to 1,2,3,4,10,10a,-hexahydropyrazino[1,2-a] indole derivatives as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R8 have the significance given in claim 1 be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnea.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H135NO – PubChem

 

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An air-stable Cu-carboxylate MOF complex can catalyze the cross-coupling reaction of phenylacetylene with 2-oxazolidone and Henry reaction. The Cu-carboxylate MOF encapsulated magnetic beads (MOF-MB II) was also prepared. The MOF-MB II was successfully reused in the Henry reaction by a simple magnetic separation. Georg Thieme Verlag Stuttgart · New York.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H311NO – PubChem

 

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By employing N-heterocyclic carbenes (NHCs) as catalysts, the carboxylative cyclization of propargylic amines proceeded under atmospheric pressure of CO2 (0.1 MPa) to afford the corresponding 2-oxazolones as the main products. It was considered that the carboxylative cyclization of propargylic amines with CO2 proceeded to initially provide 2-oxazolidinones, after which the generated 2-oxazolidinones were consecutively tautomerized to give the corresponding 2-oxazolones. Moreover, we could perform the NHC-catalyzed carboxylative cyclization of propargylic amines to provide 2-oxazolidinones or 2-oxazolones selectively under controlled reaction conditions.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H535NO – PubChem

 

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The samarium diiodide-promoted reduction of 2-deoxy-2-acetamidogalactosyl pyridyl sulfone alpha-5 with ketones or aldehydes under Barbier conditions led unexpectedly to the stereoselective synthesis of alpha-C-galactosamine derivatives in good yields. With carbonyl substrates, alpha:beta selectivities ranged from 20:1 to 5:1, and with aldehydes a stereoselectivity of approximately 5:1 was observed at C7 in favor of the S-isomer. The stereochemical preference of these C-glycosylation reactions is explained by the intermediacy of an alpha-oriented anomeric glycosyl samarium(III) compound that is stabilized via chelation of the metal ion to the C2-acetamido group.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1079NO – PubChem

 

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Nickel(0)-promoted carboxylation of N-allenylamides (allenamides) with carbon dioxide proceeded via a nickelalactone intermediate to give beta-amino acid derivatives. It was also found that the regioselectivity at the oxidative addition stage was strongly affected by the substituents on the allene part. Georg Thieme Verlag Stuttgart. New York.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H948NO – PubChem

 

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In this paper, standard molar energies of combustion of 2-oxazolidinone and 3-acetyl-2-oxazolidinone are reported. The experimental values, obtained from static-bomb combustion calorimetry, are ?(1465.42 ± 0.52) kJ·mol?1and ?(2350.86 ± 0.84) kJ·mol?1, respectively. Using these combustion energy values, the standard molar enthalpies of formation, in crystalline phase, for the aforesaid compounds were calculated. These values were also determined, and the corresponding values are ?(430.30 ± 0.96) kJ·mol?1and ?(617.72 ± 1.58) kJ·mol?1, respectively. The standard molar enthalpies of sublimation at T = 298.15 K were experimentally obtained by using the well-known Knudsen effusion method. The obtained values are (84.20 ± 3.22) kJ·mol?1and (82.36 ± 1.84) kJ·mol?1, respectively. From the above experimental results, the standard molar enthalpies of formation in gas-phase of the compounds were derived. The values are: ?(346.10 ± 3.36) kJ·mol?1and ?(535.36 ± 2.43) kJ·mol?1, respectively. To support the consistency of the experimental results presented here, enthalpies of formation in gas-phase, using the G4 composite method, were carried out as well. Experimental results suggest that the formation of intermolecular hydrogen bonds between the nitrogen (at ring’s position 3, see Fig. 1) with the oxygen (at ring’s position 2, see Fig. 1) contributes to the values of temperature and enthalpy of fusion, enthalpy of sublimation, and enthalpy of formation in solid phase.

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Oxazolidine – Wikipedia,
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(Chemical Equation Presented) A series of 4-bicyclic heteroaryl 1,2,3,4-tetrahydroisoquinoline inhibitors of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) was discovered. The synthesis and structure-activity relationship (SAR) of these triple reuptake inhibitors (TRIs) will be discussed. Compound 10i (AMR-2), a very potent inhibitor of SERT, NET, and DAT, showed efficacy in the rat forced-swim and mouse tail suspension models with minimum e ffective doses of 0.3 and 1 mg/kg (po), respectively. At efficacious doses in these assays, 10i exhibited substantial occupancy levels at the three transporters in both rat and mouse brain. The study of the metabolism of 10i revealed the formation of a significant active metabolite, compound 13.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H764NO – PubChem

 

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A new synthesis of beta-branched carboxylic acid derivatives by the 1,4-addition of dialkylaluminium chlorides to alpha,beta-unsaturated N-acyl amides, the oxazolidones (1) and the oxazinone (4), is described.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H714NO – PubChem

 

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The composition of aqueous solution of monoethanolamine used in various units of gas treatment of the Omsk Oil-Refining Plant, Joint-Stock Company, was studied by the 13C NMR spectroscopy. The components of the gases to be purified and the reactions producing the impurities were established.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1041NO – PubChem

 

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(Chemical Equation Presented) A diverse array of oxometallic species were examined as catalysts in nucleophilic acyl substitution (NAS) reactions of methyl (or ethyl) esters with protic nucleophiles. Among them, oxotitanium acetylacetonate (TiO(acac)2) and vanadyl chloride (VOCl 2-(THF)x) served as the most efficient and water-tolerant catalysts. Transesterifications of methyl and/or ethyl esters with functionalized (including acid- or base-sensitive) 1 and 2 alcohols can be carried out chemoselectively in refluxed toluene or xylene in a 1:1 substrate stoichiometry using 1 mol % catalyst loading. The resultant products were furnished in 85-100% yields by simple aqueous workup to remove water-soluble catalysts. The new NAS protocol is also amenable to amines and thiols in 74-91% yields, albeit with higher loading (2.5 equiv) of protic nucleophiles. Representative examples of commercial interests such as Padimate O and antioxidant additives for plastics were also examined to demonstrate their practical applications. A 1:1 adduct between TiO(acac)2 and a given 1-octadecanol was identified as (C18H37O) 2Ti(acac)2 and was responsible for its subsequent NAS of methyl esters.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H420NO – PubChem