- Preparation method of medicine for treating bile duct cancer
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The invention belongs to the field of medical industry, and discloses a preparation method of a medicine for treating bile duct cancer. The preparation method of the drug Varlitinib for treating bileduct cancer comprises the following steps: with 2-amino-5-nitrobenzoic acid as a starting material, carrying out cyclization and chlorination on 2-amino-5-nitrobenzoic acid and methylimidazole acetateso as to synthesize an intermediate I; with 2-chloro-5-nitrophenol as a starting material, carrying out 2-chloromethylthiazole substitution and nitro reduction to synthesize an intermediate II; with1-amino-2-propanol as a starting material, carrying out a cyclization reaction of BTC, and carrying out chlorination to synthesize an intermediate III; and carrying out C-N coupling and nitro reduction on the intermediate I and the intermediate II, and finally carrying out a C-N coupling reaction on the intermediate I and the intermediate II and an intermediate III to synthesize Varlitinib. The method is simple and convenient to synthesize, short in route, economical in raw materials, high in yield, friendly to environment and suitable for industrial production.
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Paragraph 0017; 0029; 0033; 0035
(2020/08/23)
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- Design, synthesis and bioactivities evaluation of novel quinazoline analogs containing oxazole units
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A novel type of quinazoline derivatives, which were designed by the combination of quinazoline as the backbone and oxazole scaffold as the substituent, have been synthesized and their biological activities were evaluated for anti-proliferative activities and EGFR inhibitory potency. Compound 12b demonstrated the most potent inhibitory activity (IC 50=0.95 μmol/L for EGFR), which could be optimized as a potential EGFR inhibitor in the further study. The structures of the synthesized quinazoline analogs and all intermediates were comfirmed by 1H and 13C NMR, 2D NMR spectra, IR spectra and MS spectra. Copyright
- Hou, Xuehui,Zhang, Jingyu,Zhao, Xuan,Chang, Liming,Hu, Ping,Liu, Hongmin
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supporting information
p. 538 - 544
(2014/07/08)
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