Lin Ronghui, Hoerr David C, Weaner Larry E, Salter Rhys
Janssen Research & Development LLC, Janssen Pharmaceutical Companies of Johnson & Johnson, Spring House, Pennsylvania, USA.
J Labelled Comp Radiopharm. 2017 Nov;60(13):616-623. doi: 10.1002/jlcr.3542. Epub 2017 Sep 18.
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.
卡格列净（Invokana，JNJ - 28431754）是一种口服生物可利用的选择性SGLT2（2型钠葡萄糖转运蛋白）抑制剂，已被批准用于治疗2型糖尿病。在此，我们报告了碳-13和碳-14标记的卡格列净的合成。稳定同位素标记的[¹³C]卡格列净以[¹³C]标记的葡萄糖为起始原料，经过4步合成。[¹⁴C]标记的卡格列净是通过将[¹⁴C]引入该化合物噻吩环和苯环之间的苄基位置而合成的。本文报道了同位素标记化合物的详细合成过程。
