偕二氟亚甲基的双官能团化及其在ADCs药物含氟Linker方面的应用研究

2014年，项目课题组首次提出了“含氟Linker”（含氟偶联物，可用于ADCs药物的合成）的设想。在随后的两年时间里，对偕二氟亚甲基的双侧官能团化进行了初步探索并取得了一定的进展。本项目研究基于上述研究基础，综合利用过渡金属参与的优势，进一步全面深入地研究含偕二氟亚甲基结构单元的直链烷烃的构建方法，并参考目前ADCs药物所使用的Linker的结构特点，模拟合成一些具有特定结构特征的含氟Linker前体，为后续研究奠定基础。

In 2014, our group revealed a new the concept of "containing fluorine linker" (fluorinated conjugates, for ADCs synthesis). In last two years, we focused on the preliminary exploration of bisfunctionalization of gem difluoromethylene and achieved initial progress. This research project will base on the above results, company with the advantages of utilization of transition metals, further focus and study in-depth on the construction of alkane chains which contain the gem difluoromethylene moiety. The linker characters of current ADCs drugs will be used as references in the synthesis of fluorinated linker as ADCs Liner precursor, which will lay the foundation and benefit the follow-up study.