54258-24-1

Upstream product

• 13626-59-0 3-methoxyisoxazole-5-carboxylic acid 

Downstream Products

• 54258-29-6 3-Methoxy-5-propionylisoxazol 
• 55704-94-4 N-Methyl-3-methoxyisoxazol-5-carboxamid 
• 2763-94-2 5-aminomethyl-3-methoxyisoxazole 
• 54258-27-4 3-Methoxy-5-(1-hydroxyiminoaethyl)isoxazol 
• 54258-31-0 3-Methoxy-5-(1-aminopropyl)isoxazol 
• 1218792-23-4 C₂₈H₂₀ClF₂N₇O₄ 
• 124953-44-2 4-(3-Methoxy-isoxazole-5-carbonyl)-piperazine-1-carbothioic acid (2-cyano-4,5-dimethoxy-phenyl)-amide 

Relevant academic research and scientific papers

NEPRILYSIN INHIBITORS

In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Practical synthesis of a potent bradykinin B1 antagonist via enantioselective hydrogenation of a pyridyl N-acyl enamide

(Chemical Equation Presented) A practical and efficient synthesis of bradykinin B1 antagonist 1 is described. A convergent strategy was utilized which involved synthesis of three fragments: 3, 6, and 7. Cross coupling of fragments 6 and 7 followed by amidation with 3 enabled efficient synthesis of 1 in 19 steps total, a 35% overall yield from commercially available pyridine 10. The key to the success of the synthesis was the development of a fluorodenitration step to install the fluorine in pyridine 7 and a catalytic enantioselective hydrogenation of N-acyl enamide 9 to set the stereochemistry.

Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles

Two series of oxazolidinone derivatives having substituted isoxazoles were synthesized and tested for antibacterial activities against several Gram-positive strains including the resistant strains of Staphylococcus and Enterococcus, such as MRSA, CRSA, MSSA and VRE. Some of them showed in vitro activities (MIC) comparable or superior to the reference compound vancomycin.