1318793-75-7

Upstream product

• 1333071-86-5 C₁₇H₁₈BrFO 
• 1206774-43-7 1-(5-bromo-2-fluorophenyl)-1-methylethanol 
• 612835-53-7 ethyl 5-bromo-2-fluorobenzoate 
• 1333071-87-6 2,3,4,6-tetra-O-acetyl-1-deoxy-1-{3-[1-(4-ethoxyphenyl)-1-methylethyl]-4-fluorophenyl}-β-D-glucopyranose 
• 32469-28-6 (3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one 
• 146328-85-0 5-bromo-2-fluoro-benzoic acid 
• 103-73-1 Phenetole 
• 90-80-2 D-Glucono-1,5-lactone 

Relevant academic research and scientific papers

PHENYL C-GLUCOSIDE DERIVATIVES, PREPARATION METHODS AND USES THEREOF

The present invention relates to a sodium glucose cotransporter 2 (SGLT2) inhibitor with a phenyl C-glucoside structure, its preparation method, a pharmaceutical composition containing the same, and its use in treating diabetes and preparing an anti-diabetes medicament. The invention provides a compound with the structure of general formula I and a pharmaceutically acceptable salt and prodrug ester thereof, wherein, the definitions of R5 and R6 are selected from the following: (1) R5=R6=Me; (2) R5=Me, R6=OMe; (3) R5=Me, R6=H; (4) R5=Me, R6=F; (5) R5=F, R6=H; and (6) R5=OMe, R6=H.

PHENYL C-GLUCOSIDE DERIVATIVES, PREPARATION METHODS AND USES THEREOF

The present invention relates to a sodium glucose cotransporter 2 (SGLT2) inhibitor with a phenyl C-glucoside structure, its preparation method, a pharmaceutical composition containing the same, and its use in treating diabetes and preparing an anti-diabetes medicament. The invention provides a compound with the structure of general formula I and a pharmaceutically acceptable salt and prodrug ester thereof, wherein, the definitions of R5 and R6 are selected from the following: (1) R5 = R6 = Me; (2) R5 =Me, R6 = OMe; (3) R5 =Me, R6 = H; (4) R5 =Me, R6 = F; (5) R5 = F, R6 = H; and (6) R5 = OMe, R6 = H.

Gem-dimethyl-bearing C-glucosides as sodium-glucose co-transporter 2 (SGLT2) inhibitors

Three novel gem-dimethyl C-glucosides were designed as sodium-glucose co-transporter 2 (SGLT2) inhibitors, and their syntheses started from D-glucose and three 2-substituted-5-bromobenzoic acids were achieved via a facile 8-step protocol, with the key step being anhydrous aluminum chloride-catalyzed Friedel-Crafts alkylation of tertiary alcohols and phenetol. These three SGLT2 inhibitors were evaluated in vivo with a mice oral glucose tolerance test (OGTT), and the anti-hyperglycemic activities of all these three compounds were comparable with that of the positive control Dapagliflozin. Copyright