Application of bioisostere difluoromethyl in medicinal chemistry and the research progress in its synthetic methods
10.16438/j.0513-4870.2021-0158
- VernacularTitle:生物电子等排体二氟甲基在药物化学中的应用及其化学合成方法进展
- Author:
Yin-sheng ZHANG
- Publication Type:Research Article
- Keywords:
bioisostere;
ifluoromethyl;
physicochemical property;
rug design;
synthesis
- From:
Acta Pharmaceutica Sinica
2021;56(8):2182-2196
- CountryChina
- Language:Chinese
-
Abstract:
Bioisosterism is one of the most common strategies in drug structure optimization. With the development of medicinal and organic chemistry, more and more classic and non-classical bioisosteres are used in the design of novel drugs. In recent years, fluorinated groups as a bioisostere have been paid more and more attention by pharmaceutical chemists. This paper briefly reviews the physicochemical properties, chemical preparation methods of difluoromethyl (CF2H) group, and its application in drug design to provide references for drug discovery researchers.