1.A new synthetic process of dapagliflozin
Li MA ; Menghan ZHANG ; Zhiwei XU ; Yingai SUN ; Jing ZHU ; Yingbo HUANG ; Dayong ZHANG
Journal of China Pharmaceutical University 2017;48(1):42-45
This paper describes a practical process for a SGLT2 inhibitor dapagliflozin. The target product was synthesized from 1-chloro-2-( 4-ethoxybenzyl)-4-iodobenzene and 2, 3, 4, 6-tetra-O-acetyl-alpha-D-glucopyranosyl bromide by iodine-magnesium exchange, and coupling and acetyl removing reactions with the total yield of 50%. This practical process highlights fewer reaction steps, less waste and mild reaction conditions.
2.Multiple rapid-responsive probes for hypochlorite detection based on dioxetane luminophore derivatives
Sun YINGAI ; Gao YUQI ; Tang CHUNCHAO ; Dong GAOPAN ; Zhao PEI ; Peng DUNQUAN ; Wang TIANTIAN ; Du LUPEI ; Li MINYONG
Journal of Pharmaceutical Analysis 2022;12(3):446-452
In recent years,various methods for detecting exogenous and endogenous hypochlorite have been studied,considering its essential role as a biomolecule.However,the existing technologies still pose obstacles such as their invasiveness,high costs,and complicated operation.In the current study,we developed a glow-type chemiluminescent probe,hypochlorite chemiluminescence probe(HCCL)-1,based on the scaffold of Schaap's 1,2-dioxetane luminophores.To better explore the physiological and pathological functions of hypochlorite,we modified the luminophore scaffold of HCCL-1 to develop several probes,including HCCL-2,HCCL-3,and HCCL-4,which amplify the response signal of hypo-chlorite.By comparing the luminescent intensities of the four probes using the IVIS? system,we determined that HCCL-2 with a limit of detection of 0.166 μM has enhanced sensitivity and selectivity for tracking hypochlorite both in vitro and in vivo.