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Facile synthesis of a 4-anilinoquinazoline dimer by Suzuki cross-coupling reaction
Authors:Shao Peng Chen  Yue Sun  Sheng Biao Wan  Tao Jiang
Affiliation:Key Laboratory of Marine Drugs, Chinese Ministry of Education, Shandong Provincial Key Laboratory of Glycoscience & Glycotechnology, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China
Abstract:
A novel 4-anilinoquinazoline dimer linked by a carbon-carbon bond in the C-7 position was synthesized via a one step Suzuki cross-coupling reaction. All structures of new compounds were characterized by 1H NMR, 13C NMR, and HRMS. The inhibition rate of the synthetic 4-anilinoquinazoline dimer 8 against epidermal growth factor receptor-tyrosine kinase enzymes (EGFR) in vitro was 44.4% at the concentration of 5.5 μmol/L.
Keywords:Quinazoline  Suzuki reaction  Dimer  EGFR  Synthesis  
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