Abstract
Canagliflozin (Invokana, JNJ-28431754) is an orally bioavailable and selective SGLT2 (subtype 2 sodium-glucose transport protein) inhibitor approved for the treatment of type 2 diabetes. Herein, we report the synthesis of
C and
C-labeled canagliflozin. Stable isotope-labeled [
C
]canagliflozin was synthesized in 4 steps starting from [
C
]-labeled glucose. The [
C]-Labeled canagliflozin was synthesized by incorporation of [
C] into the benzylic position between the thiophene and benzene rings of the compound. Detailed synthesis of the isotope-labeled compounds is reported.