96558-78-0,Some common heterocyclic compound, 96558-78-0, name is 3-Bromo-5-chlorophenylamine, molecular formula is C6H5BrClN, 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.
(S)-tert-Butyl l-(3-bromo-5-chlorophenylamino)-l-oxo-3-phenylpropan-2-ylcarbamate (46.D). 3-bromo-5-chlorobenzenamine (3.73 g, 18 mmol) and (S)-2-(tert- butoxycarbonyl)-3-phenylpropanoic acid (4.8g, 18 mmol) were dissolved in DMF (100 mL, 1291 mmol) then triethylmine (5 mL, 36 mmol) and HBTU (14 g, 36 mmol) were added and the mixture was stirred for 14 h. After 14 hours the reaction was diluted with 500 mL EtOAc and the organic was washed with IN HCl and saturated bicarbonate solution. The extract was concentrated under reduced pressure on a rotary evaporator to afford a residue. The residue was purified on silica eluting with EtO Ac/Hex in a linear gradient.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 3-Bromo-5-chlorophenylamine, its application will become more common.
Reference:
Patent; AMGEN INC.; DU, Xiaohui; FU, Zice; HOUZE, Jonathan, B.; JIAO, Xianyun; KIM, Yong-jae; LI, Leping; LIU, Jinqian; LIZARZABURU, Mike; MEDINA, Julio; SHEN, Wang; TURCOTTE, Simon; YU, Ming; WO2010/93849; (2010); A2;,
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