476168-17-9Relevant articles and documents
Preparation method of erlotinib intermediate
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, (2016/10/10)
The invention relates to a preparation method of an erlotinib intermediate. The method concretely comprises the following steps: 1, dissolving vanillin in an organic solvent I, adding aluminum trichloride, adding pyridine in a dropwise manner, and reacting to obtain ELTA; 2, dissolving the ELTA in an organic solvent II, adding 2-chloroethylmethyl ether, potassium carbonate and a phase transfer catalyst, and reacting to obtain ELTB; 3, adding the ELTB to water, adding an alkali and potassium permanganate, and reacting to obtain ELTC; 4, adding concentrated sulfuric acid to methanol in a dropwise manner, adding the ELTC to the above reaction system, and reacting to obtain ELTD; 5, adding concentrated sulfuric acid to concentrated nitric acid in a dropwise manner, dissolving the ELTD in an organic solvent IV, adding a prepared mixed acid to the reaction system, and reacting to obtain ELTE; 6, adding the ELTE, iron powder and ammonium chloride to an organic solvent V, adding concentrated hydrochloric acid in a dropwise manner, and reacting to obtain ELTF; and 7, adding the ELTF, trimethyl orthoformate and ammonium acetate to an organic solvent VI, and reacting to obtain the erlotinib intermediate.
Method of Synthesizing 6,7-Substituted 4-Anilino Quinazoline
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Page/Page column 7, (2010/11/03)
A method of synthesizing 6,7-substituted 4-anilino quinazoline employs 3,4-substituted benzoic acid as an initial reactant, and the 6,7-substituted 4-anilino quinazoline is obtained by an esterifying step, a nitrating step, a reducing step, a cyclizing step, and an one-pot reaction. In the above method, the initial reactant has low cost and yield. of the 6,7-substituted 4-anilino quinazoline is high, therefore, production cost can be reduced effectively, and competitive power of the product of the 6,7-substituted 4-anilino quinazoline can be improved.
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: Analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents
Wissner, Allan,Brawner Floyd,Rabindran, Sridhar K.,Nilakantan, Ramaswamy,Greenberger, Lee M.,Shen, Ru,Wang, Yu-Fen,Tsou, Hwei-Ru
, p. 2893 - 2897 (2007/10/03)
The syntheses and biological evaluations of 4-anilinoquinoline-3-carbonitrile analogues of the three clinical lead 4-anilinoquinazolines Iressa, Tarceva, and CI-1033 are described. The EGFR and HER-2 kinase inhibitory activities and the cell growth inhibition of the two series are compared with each other and with the clinical lead EKB-569. Similar activities are observed between these two series.