An improved convergent approach for synthesis of erlotinib, a tyrosine kinase inhibitor, via a ring closure reaction of phenyl benzamidine intermediate

…, A Aghanejad, JS Mojarrad

Index: Asgari, Davoud; Aghanejad, Ayuob; Mojarrad, Javid Shahbazi Bulletin of the Korean Chemical Society, 2011 , vol. 32, # 3 p. 909 - 914

Full Text: HTML

Citation Number: 6

Abstract

Abstract 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 ...