Category: 97859-49-9

On June 6, 2019, Mohamed, Shahul Hameed Peer; Bharatham, Nagakumar; Katagihallimath, Nainesh; Sharma, Sreevalli; Nandishaiah, Radha; Ramachandran, Vasanthi published a patent.Product Details of 97859-49-9 The title of the patent was Preparation of anti-bacterial heterocyclic compounds. And the patent contained the following:

The title compounds I [R1 = alkyl, cycloalkyl, alkylamino, etc.; R2 = H, F, Cl, etc.; R3 = H, alkyl, F, etc.; X1 = N or CR4 (wherein R4 = H, halo, cyano, etc.); X2 = N or CR5 (R5 = H, halo, cyano, etc.); X3 = N or CR6; and X4 = CR6 when dotted line represents a bond (R6 = H, cyano, alkyl, etc.); or X3 = CH2 or O; and X4 = CH2 when dotted line represents no bond; n = 0-2; Y1 and Y2 = (independently) N or CR7 (R7 = H, halo, cyano, etc.); Z1 = O, S, NH, CH2; R8 = H, OH, alkyl, F] along with their stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms, and pharmaceutically active derivatives thereof, useful for killing or inhibiting the growth of a microorganism selected from the group consisting of bacteria, virus, fungi, and protozoa, were prepared E.g., a multi-step synthesis of (S)-II, starting 6-methoxy-1,5-naphthyridin-4-ol and chloro(chloromethyl)dimethylsilane, was described. Exemplified compounds I were tested for their antibacterial activity (data given). Pharmaceutical compositions comprising compound I, alone and in combination with at least one antibiotic, were disclosed. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Product Details of 97859-49-9

The Article related to heterocyclic compound pyridooxazinone pyrazinooxazinone preparation antibacterial antiviral antifungal protozoacide, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Product Details of 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On July 3, 2014, Yang, Yushe; Guo, Bin; Li, Zhan; Li, Wei published a patent.Synthetic Route of 97859-49-9 The title of the patent was Benzoxazine-oxazolidinone compounds as antiinfective agents and their preparation, pharmaceutical compositions and use in the treatment of multidrug resistant bacterial infections. And the patent contained the following:

Disclosed are benzoxazine-oxazolidinone compounds of formula I and their optical isomers, pharmaceutically acceptable salts, preparation method and application in preparing drugs for treating an infectious disease and in particular, an infectious disease caused by multidrug resistant bacteria. Compounds of formula I wherein R1 is amino and derivatives, phosphonate, succinate, L-arginine; R2 is (un)branched alkyl; R3 is halo, CN, OH, amino and derivatives, etc.; and their optical isomers, pharmaceutically acceptable salts thereof, are claimed. Compounds of formula I were prepared by using cross-coupling as the key steps. All the invention compounds were evaluated for their antibacterial activity. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Synthetic Route of 97859-49-9

The Article related to benzoxazine oxazolidinone preparation antiinfective treatment multidrug resistant bacterial infection, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Synthetic Route of 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On November 28, 2017, Lu, Hualong published a patent.Electric Literature of 97859-49-9 The title of the patent was Preparation of oxazolidinone compounds as antibiotic agents. And the patent contained the following:

The title compounds shown in general formula I [wherein, R1 is selected from the groups as 3-amino-pyrrolidin-1-yl, N-methyl-3-amino-piperidin-1-yl, (R)-3-aminohexahydroazepin-1-yl, N-methyl-piperazin-1-yl, 3-methyl-piperazin-1-yl, pyrrol-1-yl, 3-methylpyrrol-1-yl, etc.; R2 is selected from H, hydroxy, Me, halogen, etc.; R3 is selected form OH, NHCOCH3, etc.] or pharmaceutically acceptable salts or isomers thereof were prepared as antibiotic agents. For example, compound II was prepared in a multi-step synthesis. The inventive compound can be applied in preparing the drugs for treating microbial infection, and II showed antibacterial activities against both Staphylococcus aureus and Staphylococcus epidermidis with MIC values of 0.25 μg/mL. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Electric Literature of 97859-49-9

The Article related to preparation oxazolidinone antibiotic agent treatment human bacterial infection, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature of 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On May 20, 1987, Hamaguchi, Shigeki; Katayama, Kazuhiko; Ohashi, Takehisa; Watanabe, Kiyoshi published a patent.Computed Properties of 97859-49-9 The title of the patent was Optically active 5-[(sulfonyloxy)methyl]-2-oxazolidinone derivatives as intermediates for drugs. And the patent contained the following:

The title compounds (I; R = SO2R1 where R1 = aryl), useful as intermediates for drugs, e.g., β-blockers, were prepared in good yield and with high optical purity by reaction of optically active crude I (R = H), which was prepared via stereospecific hydrolysis of I (R = COR2 where R2 = C7 or C8 alkyl) by a lipase from Pseudomonas aeruginosa with R1SO2X (X = halo) in the presence of a base in an inert solvent. p-MeC6H4SO2Cl (20 g) was added to a mixture of 14.6 g crude (S)-I (R = H) (80% purity) and 11 g Et3N in CH2Cl2 and the mixture was allowed to react at room temperature for 6 h to give 75% crystalline (S)-I (R = SO2C6H4Me-p). The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Computed Properties of 97859-49-9

The Article related to lipase asym hydrolysis hexanoyloxymethyloxazolidinone, chiral sulfonyloxymethyloxazolidinone preparation intermediate beta blocker, oxazolidinone preparation intermediate drug and other aspects.Computed Properties of 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On August 31, 2006, Hattori, Kazuo; Niizuma, Satoshi; Masubuchi, Miyako; Koyama, Kohei; Kondoh, Osamu; Tsukaguchi, Toshiyuki; Okada, Takehiro published a patent.Product Details of 97859-49-9 The title of the patent was Preparation of 1-(2H)-isoquinolone derivatives as antitumor agents. And the patent contained the following:

The title compounds represented by the formula (I), prodrugs thereof, or pharmaceutically acceptable salts of either of them [X = each optionally substituted aryl or heteroaryl; ring Cy = optionally substituted 4-7 membered single heterocyclic ring or 8-10 membered fused heterocyclic ring; Z = O, S, Ra; Ra= H, C1-8 alkyl, aryl-C1-6 alkyl, aryl, heteroaryl]. These compounds are useful for effectively treating and preventing proliferative diseases such as cancers, in particular solid tumors. Thus, ring-opening amination of (R)-glycidol with 7-amino-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one in ethanol under refluxing for 3 days gave 63% 7-((R)-2,3-dihydroxypropylamino)-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one which underwent cyclocondensation with di-Et carbonate in the presence of NaOMe in methanol at 105° for 13 h to give 78% 7-((S)-5-Hydroxymethyl-2-oxooxazolidin-3-yl)-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one. The representative compounds I showed IC50 of 0.021-0.96 against the proliferation of human colon cancer HCT116 cells. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Product Details of 97859-49-9

The Article related to isoquinolone preparation antitumor, proliferative disease cancer solid tumor treatment prevention isoquinolone preparation, oxooxazolidinylphenylisoquinolinone preparation antitumor and other aspects.Product Details of 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On March 14, 2002, Madar, David J.; Pireh, Daisy; Kopecka, Hana; Djuric, Steven W.; Wiedeman, Paul E. published a patent.Quality Control of (R)-5-(Hydroxymethyl)oxazolidin-2-one The title of the patent was Preparation of oxazolidinones as antibacterial agents. And the patent contained the following:

The preparation of oxazolidinones [I; wherein A = Ph, five- or six-membered ring containing 1-3 atoms selected from N, O, and S; B = heterocycle; X = O, S, S(O), SO2, and NR5 (where R5 = H, alkyl, arylalkyl); R1, R2, independently = H, alkoxy, alkyl, amino, cycloalkyl, halo, etc.; R3 = H, alkoxy, alkyl, amino aryl, etc.; R4 = alkanoyl, alkoxycarbonyl, amido, aryl, etc.] is described. Thus, a multistep synthesis of N-[[(5S)-3-[3-fluoro-4-[(E)-[2-oxo-1,2-dihydro-3H-pyrrolo(2,3-b)pyridin-3-ylidene]methyl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide is given. The prepared compounds are useful as, inter alia, antibacterial agents, inhibiting the growth of bacteria with min. inhibitory concentrations in a range of about 2 μg/mL to about 8 μg/mL. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Quality Control of (R)-5-(Hydroxymethyl)oxazolidin-2-one

The Article related to oxazolidinone preparation antibacterial, psoriasis treatment preparation oxazolidinone, antiarthritic preparation oxazolidinone, chemotherapy toxicity treatment preparation oxazolidinone and other aspects.Quality Control of (R)-5-(Hydroxymethyl)oxazolidin-2-one

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On March 28, 2013, Guo, Bin; Fan, Houxing; Xin, Qisheng; Chu, Wenjing; Wang, Hui; Huang, Yanqin; Chen, Xiaoyan; Yang, Yushe published an article.Application In Synthesis of (R)-5-(Hydroxymethyl)oxazolidin-2-one The title of the article was Solubility-Driven Optimization of (Pyridin-3-yl) Benzoxazinyl-oxazolidinones Leading to a Promising Antibacterial Agent. And the article contained the following:

The solubility-driven structural modification of substituted (pyridin-3-yl)-containing hydrobenzo[b]oxazolo[3,4-d][1,4]oxazinones is described, which resulted in the development of a new series of benzo[b]oxazolo[3,4-d][1,4]oxazinone analogs with high antibacterial activity against Gram-pos. pathogens, including that against linezolid-resistant strains, and low hERG inhibition. With regard to structure-activity relationship (SAR) trends among the various substituents on the pyridyl ring, relatively small and nonbasic substituents were preferable to sterically demanding or basic substituents. Oxazolidinone ring substitution on the pyridyl ring generated analogs with antibacterial activity superior to imidazolidinone ring. Solubility was enhanced by the incorporation of polar groups, especially when compounds were converted to their prodrugs. Among the prodrugs, compound I exhibited excellent solubility and a good pharmacokinetic profile. In a MRSA systemic infection model, compound I displayed an ED50 = 5.00 mg/kg, a potency that is 2-fold better than that of linezolid. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Application In Synthesis of (R)-5-(Hydroxymethyl)oxazolidin-2-one

The Article related to oxazolooxazinone pyridyl substituted preparation solubility driven optimization antibacterial activity, antibacterial activity sar gram pos bacteria oxazolooxazinone herg inhibition, sodium phosphate prodrug solubility pharmacokinetic and other aspects.Application In Synthesis of (R)-5-(Hydroxymethyl)oxazolidin-2-one

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On May 24, 2004, Pallavicini, Marco; Bolchi, Cristiano; Di Pumpo, Raffaella; Fumagalli, Laura; Moroni, Barbara; Valoti, Ermanno; Demartin, Francesco published an article.Reference of (R)-5-(Hydroxymethyl)oxazolidin-2-one The title of the article was Resolution of 5-hydroxymethyl-2-oxazolidinone by preferential crystallization and investigations on the nature of the racemates of some 2-oxazolidinone derivatives. And the article contained the following:

After ascertaining its conglomerate nature by DSC and solid-state IR analyses, 5-hydroxymethyl-2-oxazolidinone (I), whose enantiomers are very important synthons, was efficiently resolved without chiral auxiliaries by preferential crystallization from a supersaturated isopropanolic solution of (±)-I, slightly enriched in one enantiomer (3.7% ee). Favorable conditions to the entrainment were defined utilizing a previously constructed ternary phase diagram of (R)-I, (S)-I, and 2-propanol. Furthermore, the investigations were extended to other chiral 2-oxazolidinones with a functionalized Me at the 5- or 4-position finding that 5-[(tosyloxy)methyl]-2-oxazolidinone is a racemic compound, whereas just the corresponding mesylate is a conglomerate as the parent alc. I. Interestingly, 4-(hydroxymethyl)-2-oxazolidinone proved to be a racemic compound in contrast with its positional isomer I demonstrating how a relatively fine variation in the mol. structure can unpredictably influence the crystalline nature of the racemate. The X-ray structure determination carried out on (S)-(+)-I, (±)-4-(hydroxymethyl)-2-oxazolidinone and (R)-(+)-4-(hydroxymethyl)-2-oxazolidinone enlightened the importance of the hydrogen bond in determining different supramol. assembling in the two homochiral compounds with respect to the racemic one and allowed a correlation with the stability of the crystal to be made. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Reference of (R)-5-(Hydroxymethyl)oxazolidin-2-one

The Article related to hydroxymethyl oxazolidinone resolution preferential crystallization, phase diagram hydroxymethyl oxazolidinone resolution preferential crystallization, differential scanning calorimetry hydroxymethyl oxazolidinone resolution preferential crystallization and other aspects.Reference of (R)-5-(Hydroxymethyl)oxazolidin-2-one

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On January 10, 2008, Ryono, Dennis E.; Cheng, Peter T. W.; Bolton, Scott A.; Chen, Sean S.; Shi, Yan; Meng, Wei; Tino, Joseph A.; Zhang, Hao; Sulsky, Richard B. published a patent.Category: oxazolidine The title of the patent was Novel N-heterocyclic phosphonates and phosphinates as glucokinase activators for treatment of Type II diabetes. And the patent contained the following:

Nitrogen heterocyclic phosphorus amidoesters Y-XCONH(QR4R5R6) [1; Q = optionally substituted 2-N-heterocyclyl; R4 = optionally (5-7-membered heterocyclic) ω-phosphonoalkyl, ω-[(organyloxy)phosphinyl]alkyl, ω-phosphonatoalkyl, ω-phosphinatoalkyl, ω-phosphinylalkyl; R5, R6 = H, alkyl, halo, carboxy; X = substituted methylene, imino, vinylidene, cyclopropylidene, N-heterocyclic group, imidazolylmethyl, isoindolylmethyl, 3-indolylmethyl; Y = (hetero)aralkyl, (hetero)aryl, H], useful as activators of mice and human glucokinase for treatment of Type II diabetes, were prepared by combination of amidation, phosphonylation, alkylation, esterification and heterocyclization reactions of suitable precursors. Preferably, the compounds 1 have the structure of RXCONHQ1X1P(O)R2R3 [R = iPr, 4-MeSO2C6H4, 4-(cyclopropylsulfonyl)phenyl, PhCH2CHMe, PhCH2CH2, 5-(methylsulfonyl)-2-pyrazinyl, 1-(methylsulfonyl)-4-piperidinyl, 5-(1-azetidinylcarbonyl)-2-pyrazinyl; X = 2-cyclopentylethylidene, 4-tetrahydropyranyl-2-ethylidene, 5-(MeOCH2CHMeO)-1,3-OC6H3, 5-(iPrO)-1,3-OC6H3, 5-(1-pyrrolidinylcarbonyl)-1,3-OC6H3, 5-(2-pyridinyloxy)-1,3-OC6H3, 5-(2-pyrimidinyloxy)-1,3-OC6H3, 5-(2-pyrazinyloxy)-1,3-OC6H3; Q1 = 2-thiazol-5-yl, 2-pyridin-5-yl, 2-pyrazin-5-yl, 2-thiazol-4-yl, 2-pyridin-6-yl, 3-pyrazol-1-yl; X1 = bond, CH2, CH2CH2, CH:CH; R2 = R3 = OEt, OMe, OiPr; R3 = OEt, R4 = Me; X1P(O)R3R4 = CH2OP(O)Me2; P(O)R3P4 = 2-oxo-1,3,2-dioxaphosphorin-2-yl]. The prepared compounds 1 were tested in vitro for glucokinase activation and in vivo in diet-induced obese mice for oral glucose tolerance. In an example, amidothiazolylmethyl-substituted cyclic phosphonate, 2-RCH2-2-oxo-1,3,2-dioxaphosphorinane [169, R = 2-[4-MeSO2C6H4[5-(MeOCH2CHMeO)-1,3-OC6H3CONH]-thiazol-4-yl]] was prepared by heterocyclization of 2-BocNH-thiazol-4-ylmethylphosphonic acid bis(trimethylsilyl) ester with 1,3-propanediol, followed by deprotection and coupling with 3-[(1S)-2-methoxy-1-methylethoxy]-5-(4-methylsulfonylphenoxy)benzoic acid with 28% yield. In another example, the compound 169 exhibited 50% activation of human glucokinase at 12 mM of glucose at concentration (EC50) of 9 nM. The compounds of the invention also caused 62-80% reduction in glucose AUC level in diet-induced obese (DIO) mice at 30 mg/kg dose by oral administration. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Category: oxazolidine

The Article related to phosphonate phosphinate heterocyclic pyridinyl pyrazinyl thiazolyl preparation glucokinase activator, benzeneacetamide pyridinyl thiazolyl pyrazinyl phosphonate phosphinate preparation glucokinase activator, diabetes treatment glucokinase activator heterocyclic sulfonyl benzeneacetamide phosphonate phosphinate and other aspects.Category: oxazolidine

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On March 7, 2002, Sciotti, Richard J.; Djuric, Steven W.; Pliushchev, Marina published a patent.HPLC of Formula: 97859-49-9 The title of the patent was Preparation of oxazolidinone chemotherapeutic agents. And the patent contained the following:

Compounds of the formula I [A = Ph, substituted five-membered aromatic ring containing 1 or 2 atoms selected from N, O, and S and the remaining atoms are carbon, or substituted 6-membered aromatic ring containing 1 or 2 nitrogen atoms and the remaining atoms are carbon; R1, R2 = independently H, alkyl, cycloalkyl, hydroxy, amino, halo, haloalkyl, and perfluoroalkyl; R3 = optionally substituted alkyl, alkanoyl, carboxamido, cycloalkyl, cyclothioalkoxy, etc.; R4 = substituted N, O, or S] or therapeutically acceptable salts or prodrugs thereof were prepared Thus, Me 4-((4-((5S)-5-((acetylamino)methyl)-2-oxo-1,3-oxazolidin-3-yl)-2-fluorophenyl)ethynyl)benzoate (II) was synthesized in 6 steps from (5R)-5-(hydroxymethyl)-1,3-oxazolidin-2-one (III). Oxazolidinones of formula I are useful for treating bacterial infections, psoriasis, arthritis, and toxicity due to chemotherapy. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).HPLC of Formula: 97859-49-9

The Article related to oxazolidinone chemotherapeutic agent asym synthesis chemotherapy toxicity treatment method, psoriasis treatment method oxazolidinone chemotherapeutic agent asym synthesis, arthritis treatment method oxazolidinone chemotherapeutic agent asym synthesis, bacterial infection treatment method oxazolidinone chemotherapeutic agent asym synthesis and other aspects.HPLC of Formula: 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem