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N-4- (4 - chloro- 3 -trifluoromethyl -phenyl ) -7 - methoxy - quinazoline -4, 6-diamine (1) exhibited potential biological activities in medicine, 4-chloro-7-fluoro-6-nitro-quinazoline (2) is an important intermediate in compound 1. In this work, a rapid synthetic method for compound 1 was established. The compound 1 was synthesized from the commercially available 4-chloro-7-fluoro-6-nitro-quinazoline 2 through three steps including substitution with phenylamine, nucleophilic substitution reaction and reduction reaction. The structures were confirmed by 1 HNMR. Furthermore, the synthetic method was optimized.

Synthesis of N-4-(4-chloro-3-trifluoromethyl-phenyl)-7-methoxy-quinazoline-4,6-diamine