Tag: 100-200

On October 5, 2012, Ivashkin, Pavel; Couve-Bonnaire, Samuel; Jubault, Philippe; Pannecoucke, Xavier published an article.COA of Formula: C8H15NO2 The title of the article was Asymmetric synthesis of cyclopropanes with a monofluorinated quaternary stereocenter. And the article contained the following:

New chiral fluorinated reagents (N-(dibromofluoroacetyl)oxazolidinones) were easily synthesized and used in an asym. cyclopropanation process. The Michael initiated ring closure reaction provided chiral cyclopropanes bearing a fluorinated quaternary stereocenter. Various electron-deficient alkenes can be used to efficiently obtain chiral polysubtituted fluorinated cyclopropanes in good yields. Moderate to very good cis/trans ratios were obtained with a high level of diastereoselectivity for each isomer. 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 fluorocyclopropane enantioselective preparation, dibromofluoroacetyl oxazolidinone preparation acrylate asym cyclopropanation, Alicyclic Compounds: Cyclopropanes and other aspects.COA of Formula: C8H15NO2

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On May 3, 2018, Huang, Hui; Lanter, James C.; Meegalla, Sanath K.; Player, Mark R. published a patent.Recommanded Product: 168297-86-7 The title of the patent was Preparation of cyclohexyl derivatives as GPR40 agonists for the treatment of type II diabetes. And the patent contained the following:

Disclosed are compounds of formula I, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Compounds of formula I wherein G is 5-C1-3 alkoxy-2-fluorophenyl, 2-C1-3 alkoxy-5-fluoropyridin-4-yl, 6-methoxypyrazin-2-yl-4-methoxypyrimidin-2-yl, 2-ethyl-5-fluorophenyl and 2-ethyl-5-fluoropyridin-4-yl; R1 is H, OH, MeO and F; Ra is H and C1-4 alkyl; L is OCH2, NHCH2, CH2CH2 and CH:CH; ring W is Ph and pyridinyl; R2 is C3-5 cycloalkyl, methoxyacetylenyl, and EtO; R3 is H, Me, CF3 and F; A is carboxy and 1H-tetrazol-5-yl; and enantiomers, diastereoisomers and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The example compounds were evaluated for their GPR40 agonistic activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 0.0005 μM tp 0.0028 μM. 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 cyclohexyl derivative preparation gpr40 agonist treatment diabetes type ii, Alicyclic Compounds: Cyclohexanes and other aspects.Recommanded Product: 168297-86-7

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On May 31, 1985, Hamaguchi, Shigeki; Yamamura, Hiroshi; Hasegawa, Junzo; Watanabe, Kiyoshi published an article.Product Details of 97859-49-9 The title of the article was Biological resolution of racemic 2-oxazolidinones. Part IV. Enzymic resolution of 2-oxazolidinone esters. And the article contained the following:

The asym. hydrolysis was investigated of (R,S)-5-butanoyloxymethyl-3-phenyl-2-oxazolidinone (I) and (R,S)-5-hexanoyloxymethyl-2-oxazolidinone (II) by lipoprotein lipase from Pseudomonas aeruginosa. Lipoprotein lipase had the ability to hydrolyze racemates of I and II enantioselectively, but had no enantioselectivity on the hydrolysis of (R,S)-5-hexanoyloxymethyl-3-tert-butyloxazolidine and (R,S)-4-hexanoyloxymethyl-1,3-dioxolane-2-one. 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 oxazolidinone ester hydrolysis lipoprotein lipase, enzyme resolution oxazolidinone ester racemate, Biochemical Methods: Biological and other aspects.Product Details of 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On October 8, 2015, Anderson, David Randolph; Bunnage, Mark Edward; Curran, Kevin Joseph; Dehnhardt, Christoph Martin; Gavrin, Lori Krim; Goldberg, Joel Adam; Han, Seungil; Hepworth, David; Huang, Horng-Chih; Lee, Arthur; Lee, Katherine Lin; Lovering, Frank Eldridge; Lowe, Michael Dennis; Mathias, John Paul; Papaioannou, Nikolaos; Patny, Akshay; Pierce, Betsy Susan; Saiah, Eddine; Strohbach, Joseph Walter; Trzupek, John David; Vargas, Richard; Wang, Xiaolun; Wright, Stephen Wayne; Zapf, Christoph Wolfgang published a patent.Product Details of 97859-49-9 The title of the patent was Bicyclic-fused heteroaryl or aryl compounds as IRAK4 inhibitors and their preparation. And the patent contained the following:

Compounds of formula I, tautomers and pharmaceutically acceptable salts of the compounds are disclosed. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. Compounds of formula I wherein X, X’ and Y are independently CR8′, N and N+O-; provided at at least one of X, X’ and Y is N or N+O- and no more than one of X, X’ and Y is N+O-; R1 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, etc.; R2 is (un)substituted C0-3 alkyl-C3-10 cycloalkyl, (un)substituted C0-3 alkyl-C6-12 aryl, (un)substituted C0-3 alkyl-heteroaryl; R6 is CONH2 and derivatives, CO2H and derivatives, and CN; each R8 is independently H, halo, CN, OH and derivatives, SH and derivatives, etc.; R8′ is H, D, halo, CN, etc.; and pharmaceutically acceptable salts and tautomers, thereof are claimed. Example compound II was prepared by enzyme-mediated epimerization of 1-{[(2S,3S,4S)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide followed by hydrolysis. The invention compounds were evaluated for their IRAK4 inhibitory activity (some data given). 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 bicyclic heteroaryl aryl compound preparation irak4 inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Product Details of 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On January 31, 2013, Hoffmann, Matthias; Bischoff, Daniel; Dahmann, Georg; Klicic, Jasna; Schaenzle, Gerhard; Wollin, Stefan Ludwig Michael; Convers-Reignier, Serge Gaston; East, Stephen Peter; Marlin, Frederic Jacques; McCarthy, Clive; Scott, John published a patent.Synthetic Route of 97859-49-9 The title of the patent was Preparation of substituted quinolines as Syk inhibitors for therapy. And the patent contained the following:

The invention relates to substituted quinolines of formula I (wherein R1 is a (un)substituted C1-6-alkyl; R2 is halogen, (un)substituted Ph, (un)substituted five- or six-membered monocyclic heteroaryl, or (un)substituted bicyclic ring system), and their use as Syk inhibitors in the preparation of medicaments for the treatment of disease such as asthma, COPD, allergic rhinitis, allergic dermatitis and rheumatoid arthritis. Synthetic procedures for preparing I are exemplified. Example compound II was prepared by reacting intermediates 7-phenylquinolin-5-ol and (R)-4-((S)-1-hydroxyethyl)-1-((R)-1-phenylethyl)pyrrolidin-2-one and deprotecting the compound formed. The examples compounds were tested in a human Syk kinase inhibition assay, and had IC50 values ≤ 1 μmol. 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 preparation quinoline syk inhibitor therapy, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Synthetic Route of 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On March 22, 2011, Ryono, Denis E.; Cheng, Peter T. W.; Bolton, Scott A.; Chen, Sean; Shi, Yan; Meng, Wei; Tino, Joseph A. published a patent.Computed Properties of 97859-49-9 The title of the patent was Preparation of phosphonate and phosphinate pyrazolylamide glucokinase activators. And the patent contained the following:

Pyrazoloamides are provided which are phosphonate and phosphinate glucokinase activators that are useful in treating diabetes and related diseases and have the structure I (circle = pyrazoyl ring; R4 = -(CH2)n-Z-(CH2)m-PO(OR7)(OR8), -(CH2)nZ-(CH2)m-PO(OR7)R9, or -(CH2)nZ-(CH2)m-PO(R9)(R10); R5 and R6 are independently selected from H, alkyl and halogen; Y is R3(CH2)s, wherein R3 is aryl , s is 0, X is a bond; and n, Z, m, R4, R5, R6, and R7 are as defined herein; or a pharmaceutically acceptable salt thereof). 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 phosphonate phosphinate pyrazolylamide glucokinase activator preparation, Organometallic and Organometalloidal Compounds: Phosphorus Compounds and other aspects.Computed Properties of 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On December 3, 2020, Koehler, Michael Friedrich Thomas; Smith, Peter Andrew; Winter, Dana; Sow, Boubacar; Sturino, Claudio; Pelletier, Guillaume; Boudreault, Jonathan published a patent.Application of 97859-49-9 The title of the patent was Preparation of macrocyclic broad spectrum antibiotics. And the patent contained the following:

Macrocyclic compounds of formula I [R1 = H, alkyl; R2 = H, (substituted) NH2, alkyl, etc.; R3 = H, cycloalkyl, alkyl, etc.; R4 = H, alkyl; X = alkylene, arylene, etc.; Y = bond, O, S, alkylene, arylene, etc.; Z = H, halo, CN, alkoxy, alkylthio, acyl, alkyl, aryl, etc.] are prepared as antibacterial agents which have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidases SpsB and/or LepB, an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided. Thus, II was prepared, and had serum MIC value of 0.5μM against E. coli 25922. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Application of 97859-49-9

The Article related to macrocycle preparation antibacterial, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Application of 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On December 29, 2005, Merrill, Bryon A.; Haraldson, Chad A.; Kshirsagar, Tushar A.; Niwas, Shri published a patent.Electric Literature of 168297-86-7 The title of the patent was Preparation of imidazoquinoline and imidazonaphthyridine derivatives as immunomodulators of cytokine biosynthesis. And the patent contained the following:

The title imidazoquinoline and imidazonaphthyridine derivatives I [wherein R1 and R2 together form a benzene or pyridine ring which is optionally substituted with heterocyclyl; R3 and R4 = independently H or a substituent] or pharmaceutically acceptable salts thereof were prepared as immunomodulators of cytokine biosynthesis for the treatment of viral infection and cancer. For example, the compound II was prepared in a multi-step synthesis. Some of compounds I showed strong inhibitory effect on TNF-α in rat. 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 preparation imidazoquinoline imidazonaphthyridine immunomodulator cytokine antiviral agent antitumor human, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Electric Literature of 168297-86-7

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On November 30, 1985, Hamaguchi, Shigeki; Yamamura, Hiroshi; Hasegawa, Junzo; Watanabe, Kyoshi published a patent.Computed Properties of 97859-49-9 The title of the patent was Enzymic separation of optical isomers of 2-oxazolidinones. And the patent contained the following:

(R,S)-5-Acyloxymethyloxazolidin-2-ones I (R1 = H, (un)substituted aryl; R2 = (un)substituted alkyl) are treated with stereoselective esterases or microorganisms containing these enzymes to yield optically active 5-hydroxymethyloxazolidin-2-ones (II) and optically active but unreacted I (III). II and III are precursors for antibiotics. Thus, Pseudomonas aeruginosa lipoprotein lipase (L.P.L. Amano 3) 0.5 g and (R,S)-5-butanoyloxymethyloxazolidin-2-one 18.7 g were dissolved in 100 mL 0.1M phosphate buffer, pH 7.0. The mixture was stirred at 30° for 12 h. EtOAc extraction and fractionation by silica gel column chromatog. of the mixture yielded (R)-5-hydroxymethyloxazolidin-2-one and (S)-5-butanoyloxymethyloxazolidin-2-one (IV). The hydrolysis of IV (4 g) with NaOH yielded (S)-5-hydroxymethyloxazolidin-2-one (1.8 g). 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 acyloxymethyloxazolidinone optical isomer separation esterase, oxazolidinone isomer separation esterase, Fermentation and Bioindustrial Chemistry: Industrial Chemicals and other aspects.Computed Properties of 97859-49-9

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

On June 23, 2016, Musicki, Branislav published a patent.Safety of (R)-5-(Hydroxymethyl)oxazolidin-2-one The title of the patent was Preparation of benzenesulfonamide derivatives as inverse agonists of retinoid-related orphan receptor gamma. And the patent contained the following:

The invention relates to the preparation of benzenesulfonamide derivatives I, wherein q is an integer 0-3; L is a bond, CH2; R1 is alkyl, cycloalkyl, alkenyl, alkyl-cycloalkyl, alkyl-heterocycloalkyl; R2 is H, halogen, alkyl, alkenyl, alkoxy, CN; R3 is H, alkyl, NH2; R4 is H, alkyl, alkoxy, ether, alkyl-amino-alkyl; A1 is substituted amine, O, S, SO, SO2, SO(=NH), CH2, C=C, alkylidene; A2 is bond, S, SO, SO2, sulfonimide, CH(OH), C(=O)O; Q1-Q5 are independently N, alkylidene, and the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonists of retinoid-related orphan receptor gamma (RORγt). Thus, benzenesulfonamide II was prepared and tested in vitro as inverse agonist of retinoid-related orphan receptor gamma (IC50 = 100 nM – 1 μM). The invention also relates to pharmaceutical compositions comprising such compounds, as well as to the use thereof for the topical and/or oral treatment of RORγt receptor-mediated inflammatory diseases, in particular acne, psoriasis and/or atopic dermatitis. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Safety of (R)-5-(Hydroxymethyl)oxazolidin-2-one

The Article related to human interleukin acne benzenesulfonamide preparation, cosmetic atopic dermatitis psoriasis antiinflammatory receptor acne benzenesulfonamide preparation, Heterocyclic Compounds (More Than One Hetero Atom): Triazines and other aspects.Safety of (R)-5-(Hydroxymethyl)oxazolidin-2-one

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem