289686-70-0Relevant articles and documents
A 2 - (3, 5 - double - trifluoromethyl - phenyl) -2 - methyl - propionic acid preparation method
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Paragraph 0092-0096, (2019/07/08)
The invention provides a 2 - (3, 5 - double - trifluoromethyl - phenyl) - 2 - methyl - propionic acid preparation method. In particular, the use of 3, 5 - trifluoro - methyl-bromobenzene as raw materials, through Grignard - sediment reaction, Suzuki coupling reaction, to obtain 2 - (3, 5 - double - trifluoromethyl - phenyl) - 2 - methyl - propionic acid. The method of short synthetic route, raw materials are easy and the cost is low, mild reaction conditions, easy purification of products, and have high yield, is suitable for industrial mass production.
Preparation method of synthetic 2-(3,5-bis(trifluoromethyl)phenyl)-2-methyl propioric acid
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Paragraph 0039; 0041; 0051; 0053; 0055; 0065; 0069; 0079, (2018/04/03)
The invention discloses a preparation method of synthetic 2-(3,5-bis(trifluoromethyl)phenyl)-2-methyl propioric acid. S1: 3,5-bis(trifluoromethyl)bromobenzene is dissolved in an organic solvent, the solution is added dropwisely into isopropylmagnesium chloride, and a Grignard reagent is obtained; mafosfamide is dissolved in an organic solvent, the solution is added dropwisely into the Grignard reagent, in order to obtain 2-(3,5-bis(trifluoromethyl)phenyl)-2-methyl propyl-1-ketone; S2: 2-(3,5-bis(trifluoromethyl)phenyl)-2-methyl propyl-1-ketone obtained in the step S1 is dissolved in an organicsolvent, and 2-(3,5-bis(trifluoromethyl)phenyl)-2-bromo-methyl propyl-1-ketone is obtained; S3: 2-(3,5-bis(trifluoromethyl)phenyl)-2-bromo-2-methyl propyl-1-ketone obtained in the step S2 is dissolved in an organic solvent, zinc bromide is added, in order to obtain 2-(3,5-bis(trifluoromethyl)phenyl)-2-methyl methacrylate; S4: 2-(3,5-bis(trifluoromethyl)phenyl)-2-methyl methacrylate obtained in the step S3 is dissolved in an organic solvent, the solution is added into an aqueous solution of alkali, and 2-(3,5-bis(trifluoromethyl)phenyl)-2-methyl propioric acid is obtained.
Method for synthetizing Netupitant midbody impurity 2-(3,5-Bis-trifluoromethyl-phenyl) propionic acid
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Paragraph 0036; 0033; 0034; 0037, (2016/11/28)
The invention discloses a method for synthetizing a Netupitant midbody impurity 2-(3,5-bis-trifluoromethyl-phenyl) propionic acid, comprising the following steps: dissolving 2-cyano propionate and 3,5-bis-trifluoromethyl halogeno benzene into a first solvent, and performing a decarboxylation cyanomethylation reaction under the effects of a palladium catalyst and phosphorus ligands to obtain 2-(3,5-bis-trifluoromethyl-phenyl) propionitrile; adding the 2-(3,5-bis-trifluoromethyl-phenyl) propionitrile and alkali into a second solvent to generate 2-(3,5-bis-trifluoromethyl-phenyl) propionate, and then acidizing to obtain the 2-(3,5-bis-trifluoromethyl-phenyl) propionic acid. According to the method for synthetizing the Netupitant midbody impurity 2-(3,5-bis-trifluoromethyl-phenyl) propionic acid, the raw materials are cheap and easy to get, the operation is simple, the synthesis is easy, a side reaction cannot occur, and higher yield is achieved.