124244-41-3

Upstream product

• 1191-99-7 2,3-dihydro-2H-furan 
• 609-73-4 o-nitroiodobenzene 
• 577-19-5 2-nitrophenyl bromide 

Downstream Products

• 1384979-48-9 4-bromo-2-tetrahydrofuran-2-yl-aniline 
• 1384979-49-0 N-(4-bromo-2-nitro-6-tetrahydrofuran-2-yl-phenyl)-2,2,2-trifluoro-acetamide 
• 1384979-50-3 4-bromo-2-nitro-6-tetrahydrofuran-2-yl-aniline 
• 1384979-51-4 2-[5-(4-amino-3-nitro-5-tetrahydrofuran-2-yl-phenyl)pyrimidin-2-yl]propan-2-ol 
• 1384979-52-5 2-[5-(3,4-diamino-5-tetrahydrofuran-2-yl-phenyl)pyrimidin-2-yl]propan-2-ol 
• 1384979-47-8 2-(tetrahydrofuran-2-yl)aniline 
• 1384979-46-7 C₁₀H₉NO₃ 
• 1384979-45-6 C₁₀H₉NO₃ 

Relevant academic research and scientific papers

COMBINATION THERAPY COMPRISING|1 -ETHYL-3-[5-[2-{1 -HYDROXY-1 -METHYL-ETHYL}PYRIMIDIN-5-YL]-7-(TETRA HYDROFURAN-2-|YL}-1 H-BENZIMIDAZOL-2-YL]UREA AND DERIVATIVES THEREOF TO TREAT MYCOBACTERIUM|DISEASES

The present invention relates to combination therapies comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhi

Evaluation of WO2012177707 and WO2012097269: Vertex's phosphate prodrugs of gyrase and topoisomerase antibacterial agents

The two patent applications describe two novel compounds in the benzimidazole class of GyrB/ParE antibacterial agents and multiple phosphate prodrugs derived from these compounds. The new benzimidazole compounds have excellent antibacterial activity on Gram-positive strains. But like previous benzimidazoles, they have limited solubility and are highly protein bound. The phosphate prodrugs offer a drug substance with high aqueous solubility that should aid both intravenous and oral formulations. The potential utility of the prodrugs was demonstrated in efficacy studies.

PROCESS OF MAKING GYRASE AND TOPOISOMERASE IV INHIBITORS

The present application is directed to compounds, intermediates and methods for preparing compounds of formula (I) or a pharmaceutically acceptable salts thereof, wherein R is H or F, and each of R3, R4, and R5 are as defined herein. The compounds of formula (I) and pharmaceutical compositions comprising said compounds and salts inhibit bacterial gyrase and/or Topo IV and are useful in treating bacterial infections.

GYRASE AND TOPOISOMERASE IV INHIBITORS

The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.

SOLID FORMS OF GYRASE INHIBITOR (R)-1-ETHYL-3-[5-[2-(1-HYDROXY-METHYL-ETHYL)PYRIMIDIN-5-YL]-7-(TETRAHYDROFURAN-2-YL)-1H-BENZIMIDAZOL-2-YL]UREA

The present application is directed to solid forms of compounds of formula (I): and pharmaceutically acceptable salts thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutical compositions comprising said compounds and salts. These compound

Palladium-Catalyzed Synthesis of trans-2,5-Diaryltetrahydrofurans, Potent Platelet-Activating Factor Antagonists

trans-2,5-Diaryltetrahydrofurans 1-3, potent platelet-activating factor antagonists, have been synthesized regio- and stereoselectively by a three-step approach involving sequential palladium-catalyzed diarylation of 2,3-dihydrofuran and subsequent hydrog