Tag: 100-200

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 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 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 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 October 28, 2004, Burke, Martin D.; Berger, Eric M.; Kwon, Ohyun; Park, Seung Bum; Schreiber, Stuart L. published a patent.Safety of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one The title of the patent was Generation of skeletal diversity within a combinatorial library. And the patent contained the following:

The present invention provides a method of synthesizing a library of chem. compounds with skeletal diversity. Two approaches are used to create skeletal diversity within a library of chem. compounds: (1) the “”branching pathways”” (or reagent-based) approach; and (2) the “”folding pathways”” (or substrate-based) approach. Upon exposure to certain reaction conditions the members of the library undergo unique transformations into a diverse collection of mol. skeletons, which can be functionalized and derivatized further to generate a large collection of unique, natural product-like compounds A furan-based library synthesized using the folding pathways approach is provided, and a polycyclic library created using the branching pathways approach is also provided. The invention also provides materials, reagents, intermediates, and kits useful in the practice of the inventive method as well as method for screening the inventive compounds The experimental process involved the reaction of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one(cas: 168297-86-7).Safety of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one

The Article related to oxazolidinone combinatorial library stereoselective preparation solid phase synthesis, split pool synthesis skeletal diversity combinatorial chem oxazolidinone preparation, combinatorial matrix mol skeleton furan derivatization, skeletal diversity branched diels alder polycyclic combinatorial library and other aspects.Safety of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Tomas, Loic; Boije af Gennaes, Gustav; Hiebel, Marie Aude; Hampson, Peter; Gueyrard, David; Pelotier, Beatrice; Yli-Kauhaluoma, Jari; Piva, Olivier; Lord, Janet M.; Goekjian, Peter G. published an article in 2012, the title of the article was Total Synthesis of Bistramide A and Its 36(Z) Isomers: Differential Effect on Cell Division, Differentiation, and Apoptosis.Recommanded Product: 168297-86-7 And the article contains the following content:

The total synthesis of bistramide A and its 36(Z),39(S) and 36(Z),39(R) isomers shows that these compounds have different effects on cell division and apoptosis. The synthesis relies on a novel enol ether-forming reaction for the spiroketal fragment, a kinetic oxa-Michael cyclization reaction for the tetrahydropyran fragment, and an asym. crotonylation reaction for the amino acid fragment. Preliminary biol. studies show a distinct pattern of influence of each of the three compounds on cell division, differentiation, and apoptosis in HL-60 cells, thus suggesting that these effects are independent activities of the natural product. The experimental process involved the reaction of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one(cas: 168297-86-7).Recommanded Product: 168297-86-7

The Article related to bistramide a isomer preparation antitumor, cell division differentiation apoptosis differential effect bistramide a, enol ether formation total synthesis bistramide a isomer, kinetic oxa michal cyclization total synthesis bistramide a isomer, asym crotonylation total synthesis bistramide a isomer and other aspects.Recommanded Product: 168297-86-7

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On March 24, 2000, Fukuzawa, Shin-ichi; Matsuzawa, Hiroshi; Yoshimitsu, Shin-ichi published an article.Recommanded Product: (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one The title of the article was Asymmetric Samarium-Reformatsky Reaction of Chiral α-Bromoacetyl-2-oxazolidinones with Aldehydes. And the article contained the following:

The samarium(II) iodide mediated asym. Reformatskii-type reaction of chiral bromoacetyloxazolidinones I (R = Me2CH, Ph, PhCH2; R1 = H, Me, Ph) with various aldehydes R2CHO [R2 = Me2CH, Et2CH, c-C6H11, Me3C, Me(CH2)6, PhCH2CH2, Ph] was studied. A series of chiral 4-substituted 2-oxazolidinones and 5,5-disubstituted “SuperQuat” oxazolidinones were employed as chiral auxiliaries for α-bromoacetic acid. The reaction of I (R = Me2CH; R1 = H) with aldehydes R2CHO [R2 = Me2CH, Et2CH, c-C6H11, Me3C, Me(CH2)6, PhCH2CH2, Ph] gave β-hydroxy carboximides II [R = H; R1 = Me2CH; R2 = Me2CH, Et2CH, c-C6H11, Me3C, Me(CH2)6, PhCH2CH2, Ph] in 67-92% yields and in 64-99% diastereomeric excess. The majority of the reaction product derived from I (R = Me2CH; R1 = Ph) were highly crystalline; a single recrystallization of II [R = Me2CH; R1 = Ph; R2 = Me2CH, Me3C, Me(CH2)6, Ph] gave diastereomerically pure products with the β-hydroxy epimer not detectable by spectroscopic methods. The absolute configurations of the β-hydroxy carboximides were determined by comparison of the optical rotations of the corresponding known Et esters to the literature values. Hydrolytic cleavage of the appended β-hydroxy moieties from the auxiliary SuperQuats derivatives II (R = Me2CH; R1 = Me, Ph) was readily achieved under mild conditions using lithium hydroxide; the corresponding carboxylic acids and the returned SuperQuats were obtained in good yields without any evidence of racemization. The absolute configuration of the adduct derived from benzaldehyde was found to be R, with the samarium enolate formed by reduction of the bromoacetyl derivative favoring the transition state predicted from chelation control of the reagent; this is in analogy to the discussion that has been used for the corresponding titanium enolate. The stereochem. of the reaction may be explained by incorporating the Nerz-Stormes-Thornton chair transition structure model. The experimental process involved the reaction of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one(cas: 168297-86-7).Recommanded Product: (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one

The Article related to hydroxy acid nonracemic stereoselective preparation, ester beta hydroxy stereoselective preparation, hydroxyalkanoyl oxazolidinone stereoselective preparation, asym reformatskii reaction bromoacetyl oxazolidinone aldehyde, stereoselective reformatskii reaction bromoacetyl oxazolidinone aldehyde and other aspects.Recommanded Product: (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On July 31, 2010, Bourcet, Emmanuel; Fache, Fabienne; Piva, Olivier published an article.Safety of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one The title of the article was Stereocontrolled Synthesis of the Highly Functionalized Core Structure of Aurisides by Ring-Closing Metathesis. And the article contained the following:

Two approaches based on the ring-closing metathesis reaction have been explored for the synthesis of the core structure I of the marine natural products, the aurisides. The second approach, accomplished in a stereocontrolled manner, used both a Brown’s allylation and an Evans’ aldolization, and finally a transannular ketalization to deliver a highly functionalized auriside analog. The experimental process involved the reaction of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one(cas: 168297-86-7).Safety of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one

The Article related to auriside core structure stereocontrolled synthesis ring closing metathesis, allylation brown stereocontrolled synthesis auriside core structure, evans aldolization stereocontrolled synthesis auriside core structure, transannular ketalization stereocontrolled synthesis auriside core structure and other aspects.Safety of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On October 1, 2010, Lang, Kai; Park, Jongwoo; Hong, Sukwon published an article.COA of Formula: C8H15NO2 The title of the article was Development of Bifunctional Aza-Bis(oxazoline) Copper Catalysts for Enantioselective Henry Reaction. And the article contained the following:

Base-functionalized aza-bis(oxazoline) ligands were prepared to explore the concept of dual activation through the Lewis acid and a tethered tertiary amine base. The catalytic activity of the Cu complex was evaluated for the asym. Henry reaction. Compared with a corresponding unfunctionalized copper complex with external 1-benzyl-4-ethylpiperazine base, the ethylpiperazine-functionalized aza-bis(oxazoline) copper catalyst I resulted in rate acceleration (2.5 times) as well as improved enantioselectivity (72% ee vs 92% ee). The experimental process involved the reaction of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one(cas: 168297-86-7).COA of Formula: C8H15NO2

The Article related to chiral bifunctional bisoxazoline ligand preparation stereoselective henry reaction catalyst, aryl aldehyde copper chiral base functionalized ligand henry reaction, benzylic alc nitro derivative stereoselective preparation, henry reaction kinetic copper ligand base reaction order and other aspects.COA of Formula: C8H15NO2

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On December 16, 2011, Adams, Harry; Collins, Rebecca C.; Jones, Simon; Warner, Christopher J. A. published an article.Electric Literature of 168297-86-7 The title of the article was Enantioselective preparation of P-chiral phosphine oxides. And the article contained the following:

A highly efficient chiral auxiliary-based strategy for the asym. synthesis of P-chiral phosphine oxides in >98:2 er has been developed. Racemic phosphinyl chlorides undergo highly stereoselective asym. substitution with N-deprotonated chiral oxazolidinones, yielding chiral phosphinic amides, which react with Grignard reagents, giving chiral phosphine oxides. The methodol. involves the highly stereoselective formation of P-chiral oxazolidinones that then undergo displacement with a variety of Grignard reagents to prepare the desired phosphine oxides. The experimental process involved the reaction of (S)-4-Isopropyl-5,5-dimethyloxazolidin-2-one(cas: 168297-86-7).Electric Literature of 168297-86-7

The Article related to phosphine oxide chiral preparation oxazolidinone asym phosphinylation grignard reaction, substitution asym phosphinylation chiral auxiliary oxazolidinone phosphinic amide preparation, arylation alkylation phosphinic amide stereoselective preparation chiral phosphine oxide and other aspects.Electric Literature of 168297-86-7

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem