A method for the synthesis of antineoplastic

The present invention relates to an antitumor agent N- [2 - [[2- (dimethylamino) ethyl] methylamino] -4-methoxy-5 - [[4- (1-methyl -1H - indol-3-yl) -2-pyrimidinyl] amino] phenyl] -2-acrylamide (AZD9291) and key intermediates, 4-fluoro-2-methoxy-5-nitro aniline is protected by Boc anhydride to give 4-fluoro-2-methoxy-5-tert-butyl-nitroanilino, then with N, N, N'- trimethyl-ethylenediamine to give 4- (N, N, N'- trimethyl-ethylenediamine-yl) -2-methoxy-5-tert-butyl-nitroanilino, then subjected to a reduction to give 2- (N, N, N'- trimethyl-ethanediyl amino) -4-methoxy-5-tert-butyl aniline, followed by reaction with acryloyl chloride after removal of the Boc protecting group and obtain directly 2-methoxy -4-N, N, N'- trimethyl ethylenediamine-5-yl acrylamide aniline, and finally 3- (2-chloro-4-yl) -1-methyl-indole reaction with AZD9291. This process step is simple, high yield, mild reaction conditions, easy industrial production.