819813-71-3Relevant articles and documents
KINASE INHIBITORS
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Paragraph 0156, (2017/10/07)
Compounds that inhibit kinase Lck or Btk, pharmaceutically acceptable salts, hydrides, stereoisomers and pharmaceutical compositions thereof are disclosed.
Bacterial Cell Growth Inhibitors Targeting Undecaprenyl Diphosphate Synthase and Undecaprenyl Diphosphate Phosphatase
Wang, Yang,Desai, Janish,Zhang, Yonghui,Malwal, Satish R.,Shin, Christopher J.,Feng, Xinxin,Sun, Hong,Liu, Guizhi,Guo, Rey-Ting,Oldfield, Eric
supporting information, p. 2311 - 2319 (2016/10/24)
We synthesized a series of benzoic acids and phenylphosphonic acids and investigated their effects on the growth of Staphylococcus aureus and Bacillus subtilis. One of the most active compounds, 5-fluoro-2-(3-(octyloxy)benzamido)benzoic acid (7, ED50
An improved convergent approach for synthesis of erlotinib, a tyrosine kinase inhibitor, via a ring closure reaction of phenyl benzamidine intermediate
Asgari, Davoud,Aghanejad, Ayuob,Mojarrad, Javid Shahbazi
, p. 909 - 914 (2012/01/05)
An improved convergent and economical method has been developed for the synthesis of erlotinib, a 4-anilinoquinazoline and an EGFR-tyrosine kinase inhibitor for treatment of non-small-cell lung cancer. The final two steps for the formation of this 4-anilinoquinazoline from suitable 2-aminobenzonitrile intermediate and 3-ethynylaniline were modified and were performed in a simple one-pot reaction. The ring-closing mechanism for the formation of erlotinib from the suitable formamidine intermediate and 3-ethynylaniline was investigated and determined to proceed via the formation of phenyl benzamidine intermediate rather than involving Dimroth rearrangement reported earlier. The new benzamidine intermediate was isolated for the first time and characterized. Copyright