415684-05-8

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 34839-13-9 (2S)-1-amino-3-chloropropan-2-ol hydrogen chloride 
• 681225-50-3 (2S)-1-azido-3-chloropropan-2-ol 
• 34839-13-9 (S)-1-amino-3-chloro-2-propanol hydrochloride 

Downstream Products

• 777089-77-7 [(S)-3-((1S,5R,6S)-3-Fluoro-4-3-thia-bicyclo[3.1.0]hex-6-yl-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-carbamic acid tert-butyl ester 
• 777089-90-4 [(S)-3-((1S,5R,6S)-3,5-Difluoro-4-3-thia-bicyclo[3.1.0]hex-6-yl-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-carbamic acid tert-butyl ester 
• 570391-01-4 (S)-[[3-[4-(2,3-dihydro-1,1-dioxido-4H-1,4-thiazin-4-yl)-3,5-difluorophenyl]-2-oxo-5-oxazolidinyl]methyl]carbamic acid, 1,1-dimethylethyl ester 
• 847371-43-1 (3-{4-[4-(tert-butyl-dimethyl-silanyloxy)-cyclohexyl]-3-fluoro-phenyl}-2-oxo-oxazolidin-5-ylmethyl)-carbamic acid tert-butyl ester 
• 161513-47-9 (S)-<<(tert-butoxycarbonyl)amino>methyl>oxirane 
• 919357-47-4 tert-butyl {(5S)-3-[3,5-difluoro-4-(3-hydroxy-3-methylcyclobutyl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methylcarbamate 
• 919356-94-8 tert-butyl {(5S)-3-[3,5-difluoro-4-(3-methoxyazetidin-1-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methylcarbamate 
• 919357-35-0 C₂₀H₂₇F₂N₃O₅ 
• 919357-49-6 tert-butyl ((5S)-3-{3,5-difluoro-4-[3-hydroxy-3-(trifluoromethyl)azetidin-1-yl]phenyl}-2-oxo-1,3-oxazolidin-5-yl)methylcarbamate 
• 919356-96-0 tert-butyl {(5S)-3-[3,5-difluoro-4-(3-fluoroazetidin-1-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methylcarbamate 
• 919357-01-0 tert-butyl {(5S)-3-[3,5-difluoro-4-(3-{tert-butyldimethylsilyloxy}azetidin-1-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methylcarbamate 
• 919357-07-6 tert-butyl ((5S)-3-{3,5-difluoro-4-[3-(methoxyimino)azetidin-1-yl]phenyl}-2-oxo-1,3-oxazolidin-5-yl)methylcarbamate 
• 919357-28-1 tert-butyl {(5S)-3-[3,5-difluoro-4-(3-hydroxy-3-methylazetidin-1-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methylcarbamate 
• 919357-51-0 tert-butyl {(5S)-3-[-3,5-difluoro-4-(3-fluoro-3-methylazetidin-1-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methylcarbamate 

Relevant academic research and scientific papers

A fluorine-containing oxazolidinone compounds and its preparation method and application

The invention discloses a fluorine-containingoxazolidinonecompound as well as a preparation method and an application thereof. The structural formula of the fluorine-containingoxazolidinonecompound is as follows, wherein Rf refers to a trifluoromethyl group, a difluoromethyl group, a fluorine atom or perfluoralkane, R and Rindependently refer to H, C1-C6 straight-chain or branchedalkyl groups, C1-C6 straight-chain or branchedperfluoroalkyl groups, C1-C6 straight-chain or branchedalkoxygroups, a halogen such as F, Cl, Br or I, a nitro group, a cyano group or a phenyl group; R, R, R and Rindependently refer to H, F, Cl, Br, I or C1-C3 alkyl groups. The fluorine-containingoxazolidinonecompound has the better antimicrobial activity on watermelonanthracnose and cucumber grey mold and is particularly good in inhibitory activity on phytopathogencucumber grey mold of imperfect fungihyphomycetes, and a new choice is provided for development and utilization of new sterilization pesticides.

Synthesis and in vitro antibacterial activity of novel fluoroalkyl-substituted pyrazolyl oxazolidinones

A series of novel oxazolidinone derivatives bearing fluoroalkyl-substituted pyrazole as the C-ring structure were designed, synthesized and evaluated for their antibacterial activity against six Gram-positive bacterial pathogens. Most of the target compounds have good antibacterial activity. Especially, compounds 13f, 13i and 13l show excellent activity comparable to linezolid.

BH4 ANTAGONISTS AND METHODS RELATED THERETO

The disclosure relates to BH4 inhibitors and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.

2-BENZOTHIOPHENYL- AND 2-NAPHTHYL-OXAZOLIDINONES AND THEIR AZAISOSTERE ANALOGUES AS ANTIBACTERIAL AGENTS

The invention relates to antibacterial compounds of formula (I) wherein U, V, W, X, R1, R2, m, A, B and G are as defined in the description, to pharmaceutically acceptable salts of such compounds and to the use of these compounds in the manufacture of a medicament.

Stereoselective synthesis of novel (R)- and (S)-5-azidomethyl-2-oxazolidinones from (S)-epichlorohydrin: a key precursor for the oxazolidinone class of antibacterial agents

A facile synthesis of novel (R)- and (S)-5-azidomethyl-2-oxazolidinones starting from (S)-epichlorohydrin is described. The (R)-azide was utilized for the preparation of Linezolid.

ANTIMICROBIAL [3.1.0] BICYCLOHEXYLPHENYL-OXAZOLIDINONE DERIVATIVES AND ANALOGUES

The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of Formula (I) or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, an

The synthesis of N-aryl-5(S)-aminomethyl-2-oxazolidinone antibacterials and derivatives in one step from aryl carbamates

Since 1993, a significant process research and development effort directed towards the large-scale synthesis of oxazolidinone antibacterial agents has been ongoing in both Early Chemical Process Research and Development, and Chemical Process Research and Development at Pharmacia. This work has led to the successful development of the current commercial process to produce Zyvox (linezolid), recently approved by the FDA as an antibacterial. While this synthesis is appropriate for the preparation of linezolid in particular, a more convergent and versatile synthesis was developed for the rapid preparation of numerous other oxazolidinone analogues. Toward this end, economical methods for the large-scale preparation of N-[(2S)-2-(acetyloxy)-3-chloropropyl]acetamide 3 and tert-butyl [(2S)-3-chloro-2-hydroxypropyl]carbamate 27 from commercially available (S)-epichlorohydrin via the common intermediate (2S)-1-amino-3-chloro-2-propanol hydrochloride 2a were developed. Also, general methods for coupling these reagents with N-aryl carbamates to give N-aryl-5(S)-aminomethyl-2-oxazolidinone derivatives in one step were developed. These reagents and procedures have proven widely applicable in the preparation of a diverse array of oxazolidinone analogues such as 23 and 28 in both process and medicinal chemistry research.

Methods of producing oxazolidinone compounds

Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of g

Oxazolidinones having a benzannulated 6- or 7-membered heterocycle

The present invention provides oxazolidinones having a benzannelated 6- or 7-membered heterocycle as antibacterial agents.