We used 5-chloro-2-nitroaniline as a starting material and obtained the intermediate 4-AMINO-2-CHLORO-5-NITROBENZOTRIFLUORIDE in a relatively high yield through a four-step reaction involving iodination, acetylation protection, trifluoromethylation, and deacetylation. Through continuous experimentation, the yield of the trifluoromethylation step was found to be as high as 78%. The synthesis of 4-AMINO-2-CHLORO-5-NITROBENZOTRIFLUORIDE mainly involves four steps: iodination, acetylation protection, trifluoromethylation, and deacetylation. The synthetic route is shown in Figure 1.
Synthetic Route of 5-Chloro-2-nitro-4-(trifluoromethyl)aniline
Using 5-chloro-2-nitroaniline and elemental iodine as raw materials, the pesticide intermediate 4-AMINO-2-CHLORO-5-NITROBENZOTRIFLUORIDE is synthesized through a four-step reaction involving iodination, acetylation protection, trifluoromethylation, and deacetylation. This method has the following outstanding features: ① The raw materials are inexpensive and readily available; ② The reaction conditions are mild and easy to control; ③ The reaction system is simple, and the intermediate is easy to separate and purify; ④ The single-step yield is high, and the overall yield is moderate, showing potential development and application value.
