61248-83-7Relevant academic research and scientific papers
METHOD FOR PREPARING OXAZOLIDINONE INTERMEDIATE
-
, (2018/11/21)
The invention relates to a method for preparing an oxazolidinone intermediate. Specifically, a synthesis procedure for the intermediate comprises: directly performing a “one-pot” reaction on a compound I, compound J or compound L without performing isolation, wherein a salt of a compound K is selected from a hydrochloride, sulfate, malate, tartrate, p-toluenesulfonate, or lactate, and wherein the symbol * in a compound indicates an atom of an R-type chirality or an S-type chirality or a racemate thereof.
POLYCYCLIC TLR7/8 ANTAGONISTS AND USE THEREOF IN THE TREATMENT OF IMMUNE DISORDERS
-
Paragraph 00414, (2017/07/06)
The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as toll-like receptor 7/8 (TLR7/8) antagonists. In Formula (I), Ring A is aryl or heteroaryl; Ring B is aryl or heteroary; and X is C(R4)2, O, NR4, S, S(R4), or S(R4)2.
SELECTIVELY SUBSTITUTED QUINOLINE COMPOUNDS
-
Paragraph 0173; 0345, (2015/04/21)
Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
Synthesis and structure-activity relationship of a novel class of 15-membered macrolide antibiotics known as '11a-azalides'
Sugimoto, Tomohiro,Tanikawa, Tetsuya,Suzuki, Keiko,Yamasaki, Yukiko
, p. 5787 - 5801 (2012/11/06)
Macrolide antibiotics are widely prescribed for the treatment of respiratory tract infections; however, the increasing prevalence of macrolide-resistant pathogens is a public health concern. Therefore, the development of new macrolide scaffolds with activities against resistant pathogens is urgently needed. An efficient method for reconstructing the erythromycin A macrolactone skeleton has been established. Based on this methodology, novel 15-membered macrolides, known as '11a-azalides', with substituents at the C12, C13, or C4″ positions were synthesized and their antibacterial activities were evaluated. These derivatives showed promising antibacterial activities against erythromycin-resistant Streptococcus pneumoniae. Among them, the C4″ substituted derivatives had the most potent activity against erythromycin-resistant S. pneumoniae.
Synthesis and antibacterial activity of a novel class of 15-membered macrolide antibiotics, "11a-Azalides"
Sugimoto, Tomohiro,Tanikawa, Tetsuya
body text, p. 234 - 237 (2011/04/26)
An efficient method for the reconstruction of the 9-dihydroerythromycin A macrolactone skeleton has been established. The key steps are oxidative cleavage at the 11,12-position and reconstruction after insertion of an appropriate functionalized amino alcohol. Novel 15-membered macrolides, we named as "11a-azalides", were synthesized based on the above methodology and evaluated for their antibacterial activity. Among them, (13R)-benzyloxymethyl- 11a-azalide showed the most potent Streptococcus pneumoniae activity, with improved activity against a representative erythromycin-resistant strain compared to clarithromycin (CAM).
Ring-Closure Reactions through Intramolecular Displacement of the Phenylselenonyl Group by Nitrogen Nucleophiles: A New Stereospecific Synthesis of N-Tosyl and N-Benzoyl-1,3-oxazolidin-2-ones from β-Hydroxyalkyl Phenyl Selenides
Tiecco, Marcello,Testaferri, Lorenzo,Temperini, Andrea,Bagnoli, Luana,Marini, Francesca,Santi, Claudio
, p. 1752 - 1764 (2007/10/03)
A new and convenient method for the stereospecific synthesis of variously substituted 1,3-oxazolidin-2-ones from the easily available β-hydroxyalkyl phenyl selenides is presented. After transformation into the N-tosyl or N-benzoyl carbamates, the selenide
Synthesis of N-sulfonyl aziridines through regioselective opening of epoxides under solid-liquid PTC conditions
Albanese, Domenico,Landini, Dario,Penso, Michele,Petricci, Silvia
, p. 6387 - 6394 (2007/10/03)
The ring opening of epoxides 1 with 4-toluenesulfonamide (6) under solid-liquid phase transfer catalysis (SL-PTC) conditions afforded regioselectively β-sulfonamidoalcohols 7 in high yields. These were further convened into N-sulfonylaziridines 9 after ac
