1341209-29-7

Upstream product

• 1341209-27-5 (Z)-4-(5-bromo-4-fluoro-2-nitrophenoxy)but-2-en-1-ol 
• 1341209-28-6 benzyl (Z)-(4-bromo-5-fluoro-2-((4-hydroxybut-2-en-1-yl)oxy)phenyl)carbamate 
• 501-53-1 benzyl chloroformate 
• 167415-27-2 1-bromo-2,5-difluoro-4-nitrobenzene 

Downstream Products

• 1341209-34-4 [(3R,3aS)-7-bromo-8-fluoro-1-oxo-1,3,3a,4-tetrahydrobenzo[b]oxazolo[3,4-d][1,4]oxazin-3-yl]methyl 3-nitrobenzene-1-sulfonate 
• 1341209-30-0 benzyl (4-bromo-2-{[(2R,3S)-3-{[(tert-butyldimethylsilyl)oxy]methyl}oxiran-2-yl]methoxy}-5-fluorophenyl)carbamate 

Relevant academic research and scientific papers

Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis

A novel series of fluorine-containing benzoxazinyl-oxazolidinones were designed and synthesized as antidrug-resistant tuberculosis agents possessing good activity and improved pharmacokinetic profiles. Compound 21 exhibited not only outstanding in vitro a

NOVEL BENZOXAZINE OXAZOLIDINONE COMPOUNDS, PREPARATION METHODS AND USES THEREOF

Novel benzoxazine oxazolidinone compounds, preparation methods and uses thereof are disclosed, which belong to the field of pharmacy. More specifically, novel benzoxazine oxazolidinone compounds represented by the following formula (I), preparation method

Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents

A series of novel benzoxazinyl-oxazolidinones bearing nonaromatic heterocycle or aryl groups were designed and synthesized. Their in vitro and in vivo antibacterial activities were investigated. Most of the (3S, 3aS) biaryl benzoxazinyl-oxazolidinones exhibited potent activity against Gram-positive pathogens. SAR trends were observed; a pyridyl C ring was preferable to other 5- or 6-member aryl C rings, while fluorine substitution on the B ring generated derivatives with reduced activity. Various substituent group positions on the pyridyl ring were also evaluated. The resulting compounds displayed excellent activity against linezolid-resistant strains. Compound 45 exhibited excellent in vitro activity, with a MIC value of 0.25-0.5 μg/mL against MRSA and an activity against linezolid-resistant strains of 8-16-fold higher potency than linezolid. In a MRSA systemic infection model, compound 45 displayed an ED 50 5.0 mg/kg, a potency that is nearly 3-fold better than that of linezolid. This compound also showed excellent pharmacokinetic profiles, with a half-life of more than 5 h as well as an oral bioavailability of 81% in rats.