267651-24-1Relevant articles and documents
Method for synthesizing 2 - amino -5 - arylthiazole
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Paragraph 0029; 0030; 0032; 0033; 0035; 0036; 0038; 0039, (2020/07/13)
The present invention discloses a synthetic method of 2-amino-5-arylthiazole. The method is as below: dropwise adding an organometallic reagent into raw materials of 2,6-dibromo anisole and tetrahydrofuran under nitrogen protection, and stirring at room temperature or low temperature for 2 h until the materials disappear; dropwise adding a tetrahydrofuran solution containing N- methyl-N-methoxy-chloro acetamide and insulating until the disappearance of a TLC indicated intermediate; dropwise adding saturated ammonium chloride solution, separating and extracting the aqueous phase with ethyl acetate; combining the organic phases, and evaporating the solvents to obtain 2'-chloro-3-bromo-2-methoxyacetophenone; adding 2'-chloro-3-bromo-2-methoxyacetophenone, thiourea and ethanol to a reaction flask, and heating at reflux; cooling, adding into an aqueous solution of sodium bicarbonate; and filtering and drying to obtain 2-amino-5-(2'-methoxy-3'-bromo)phenyl-thiazole. The method is easy, realizes one-step synthesis of 2'-chloro-3-bromo-2-methoxyacetophenone intermediate, and utilizes the intermediate for high yield synthesis of 2-amino-5-(3'-bromo-2'-methoxy) phenylthiazole.