Downstream synthetic route of 88982-82-5

88982-82-5, 88982-82-5 4-Bromo-1,3-thiazole-2-carboxylic acid 15122065, athiazole compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.88982-82-5,4-Bromo-1,3-thiazole-2-carboxylic acid,as a common compound, the synthetic route is as follows.

Step A:4-bromothiazole-2-carboxylic acid (1,1.0 g, 4.8 mmol)Dissolved in ethylene glycol dimethyl ether (12mL)And water (4mL),Add 4-fluorophenylboronic acid (17, 1.0 g, 7.2 mmol)And anhydrous potassium carbonate (994 mg, 7.2 mmol),Then tetrakis(triphenylphosphine)palladium (277 mg, 0.24 mmol) was added.The resulting mixture was heated to 98 C under nitrogen for 24 hours.TLC analysis indicated the end of the reaction.The reaction solution was cooled to room temperature.Then add water (40 mL),The pH was adjusted to 2-3 with 6M hydrochloric acid.Filtered, the filter cake was dissolved in 20 mL of dichloromethane.The dichloromethane layer was washed with a saturated sodium bicarbonate solution.Divide the water layer,Adjust the pH of the water layer to 2-3,Filter the suspension,The filter cake was dried to give compound 18 (906 mg).Yield: 84.7%.

88982-82-5, 88982-82-5 4-Bromo-1,3-thiazole-2-carboxylic acid 15122065, athiazole compound, is more and more widely used in various fields.

Reference£º
Patent; Zhejiang Haizheng Pharmaceutical Co., Ltd.; Wang Haibo; Zheng Xiaohe; Cai Zhengjiang; Zheng Shan; Ye Zhengchun; Ma Huidan; Lin Haiming; (54 pag.)CN108623532; (2018); A;,
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