Share This Author
Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor which reduced blood glucose levels in a dose-dependent manner by as much as 55% in hyperglycemic…
In Vitro Characterization and Pharmacokinetics of Dapagliflozin (BMS-512148), a Potent Sodium-Glucose Cotransporter Type II Inhibitor, in Animals and Humans
Pharmacokinetic parameters for dapagliflozin in preclinical species revealed a compound with adequate oral exposure, clearance, and elimination half-life, consistent with the potential for single daily dosing in humans.
Synthesis and evaluation of inhibitors of bacterial D-alanine:D-alanine ligases.
Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.
Synthesis of substituted N-benzyl pyridones via an O- to N-alkyl migration.
- Erica L. Lanni, Mike Bosscher, Bartel D. Ooms, Christina A. Shandro, B. Ellsworth, Carolyn E Anderson
- ChemistryThe Journal of organic chemistry
- 9 July 2008
This LiI-promoted O- to N-alkyl migration has been developed and serves as an efficient means for the preparation of N-benzyl pyridones, quinolones, and pyrimidones.
Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.
C-Arylglucoside synthesis: triisopropylsilane as a selective reagent for the reduction of an anomeric C-phenyl ketal
A Practical Stereoselective Synthesis and Novel Cocrystallizations of an Amphiphatic SGLT-2 Inhibitor
A practical synthesis of the SGLT-2 inhibitor β-C-aryl-d-glucoside (1) has been developed. The route employed 2,3,4,6-tetra-O-trimethlysilyl-d-glucano-1,5-lactone as the key chiral building block,…
Remarkable beta-selectivity in the synthesis of beta-1-C-arylglucosides: stereoselective reduction of acetyl-protected methyl 1-C-arylglucosides without acetoxy-group participation.
An efficient and practical process to generate beta-C-arylglucoside derivatives was achieved and an unprecedented critical role of water was identified during the reduction process, made additionally efficient and highly selective.