A new synthetic process of dapagliflozin
10.11665/j.issn.1000-5048.20170106
- VernacularTitle:达格列净合成工艺的改进
- Author:
Li MA
;
Menghan ZHANG
;
Zhiwei XU
;
Yingai SUN
;
Jing ZHU
;
Yingbo HUANG
;
Dayong ZHANG
- Keywords:
SGLT2 inhibitors;
dapagliflozin;
synthesis;
process improvement;
antidiabetic agents
- From:
Journal of China Pharmaceutical University
2017;48(1):42-45
- CountryChina
- Language:Chinese
-
Abstract:
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.
