Halogen-bond-promoted direct cross-coupling of ethyl 3-bromo-3-alkyl-2,2-difluoropropanoates with coumarins/quinolinones

Author:

Pu Guoliang1,Song Shi-Yuan2,Yang Jian1,Guo Peng1,Jia Jia1,Liu Peijun1,Li Xuefei13,Liu Ping2,He Chun-Yang14ORCID

Affiliation:

1. Key Laboratory of Biocatalysis & Chiral Drug Synthesis of Guizhou Province, Generic Drug Research Center of Guizhou Province, Zunyi Medical University, Zunyi, Guizhou, P. R. China

2. Key Laboratory of Clinical Pharmacy of Guizhou Province, School of Pharmacy, Zunyi Medical University, Zunyi, Guizhou, China

3. Department of Nuclear Medicine, Affiliated Hospital of Zunyi Medical University, Zunyi, Guizhou, P. R. China

4. Key Laboratory of Basic Pharmacology of Ministry of Education and Joint International Research Laboratory of Ethnomedicine of Ministry of Education, School of Pharmacy, Zunyi Medical University, Zunyi, Guizhou, P. R. China

Abstract

A practical method for the cross-coupling of ethyl 3-bromo-3-alkyl-2,2-difluoropropanoates with coumarins/quinolinones was developed. The IC50 values of 3l against Huh-7 and A549 cells were determined to be 4.6 μM and 6.8 μM, respectively.

Funder

National Natural Science Foundation of China

Guizhou Science and Technology Department

Natural Science Foundation of Guizhou Province

Publisher

Royal Society of Chemistry (RSC)

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