Related Products of 432-21-3,Some common heterocyclic compound, 432-21-3, name is 2-Amino-6-chlorobenzotrifluoride, molecular formula is C7H5ClF3N, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
[00221] A mixture of 49.3 (50 mg, 0.134 mmol), 3-chloro-2-(trifluoromethyl)aniline (40 mg, 0.2 mmol) and aqueous Na2C03 solution (2 N, 0.80 mmol) in i-PrOH/H20 (10:1 , 4 ml_) was degassed with N2. Then Pd(PPh3)2CI2 (10 mg, 0.0134 mmol) was added to. The reaction suspension was degassed with N2 and heated at 100 C for 30 min by microwave reactor. The reaction mixture was diluted with EA and washed with water. The combined organic layers was dried over anhydrous Na2S04 and filtered. The filtrate was evaporated to give the crude which was purified by prep-HPLC (0.1 % TFA/ACN/ H20) to give the title compound (4.6 mg, 5%). 1H NMR (300 MHz, DMSO-cf6) delta ppm 7.76 (d, 2H), 7.63 – 7.53 (m, 4H), 7.31 (t, 1 H), 7.17 (dd, 2H), 6.93 (d, 1 H), 6.62 (d, 1 H), 3.85 (s, 3H), 3.63 (s, 2H). LC-MS: [M+H]+ = 407.8.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Amino-6-chlorobenzotrifluoride, its application will become more common.
Reference:
Patent; NOVARTIS AG; HE, Feng; DU-CUNY, Lei; XIAO, Qitao; XUN, Guoliang; ZHENG, Qiangang; (152 pag.)WO2017/149463; (2017); A1;,
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