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ChemicalBook CAS DataBase List 2-AMINO-5-(4-FLUOROPHENYL)-THIAZOLE
774-50-5

2-AMINO-5-(4-FLUOROPHENYL)-THIAZOLE synthesis

4synthesis methods
-

Yield:774-50-5 30%

Reaction Conditions:

with hydrogenchloride in 1,4-dioxane;water; for 6 h;Reflux;

Steps:

5d.B

General procedure: Synthesis of 2-aminothiazoles (5). Method B [0207] [0208] To a solution of N-thiazol-2-yl-acetamide (5 mmol), tripotassium phosphate (6 mmol), palladium(II)acetate (0.056 g, 0.25 mmol) and the corresponding iodide R1I (5 mmol) in anhydrous DMF (10 ml) tricyclohexyl phosphine (0.5 mmol) was added under argon. The reaction mixture was irradiated in microwave for 1 h at 140°C. After the reaction was cooled to room temperature, the reaction mixture was diluted with water (60 ml). The formed precipitate of compound 29 was filtered off and dried. [0209] A solution of 29 (10 mmol) and aqueous HCl (8 M, 100 ml) in dioxane (25 ml) was refluxed for 6 h, then cooled down to room temperature, diluted with water (100 ml) and neutralized with aqueous sodium hydroxide. The formed precipitate of thiazole 5 was filtered off, washed with water and dried.

References:

EP2719696,2014,A1 Location in patent:Paragraph 0206-0209