883267-70-7Relevant articles and documents
Novel method for preparing 2,4,5-trifluoro phenylacetic acid
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Paragraph 0046; 0047, (2017/08/29)
The invention provides a novel method for preparing 2,4,5-trifluoro-phenylacetic acid. The novel method specifically comprises the following steps: (1) dissolving 1,2,4-trifluoro benzene into 1,2-dihalogenated ethane, carrying out a Friedel-crafts alkylation reaction under catalysis of a lewis acid catalyst, thus preparing 2,4,5-trifluoro halogenated ethylbenzene; (2) hydrolyzing the 2,4,5-trifluoro halogenated ethylbenzene obtained in the step (1) in an alkaline system, thus obtaining 2,4,5-trifluoro phenethyl alcohol; (3) oxidizing the 2,4,5-trifluoro phenethyl alcohol obtained in the step (2), thus obtaining the 2,4,5-trifluoro phenylacetic acid. The novel method disclosed by the invention has the advantages that raw materials are easy to obtain, the reaction is mild, the operation is easy, the cost is low, environment friendliness is realized, no high-toxicity reagent exists, and the like.
A west he row sandbank and its salt synthesis method (by machine translation)
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Paragraph 0061; 0062; 0063; 0064; 0065, (2017/08/04)
The invention discloses a west he row sandbank and its salt synthesis method, in order to 2, 4, 5 - trifluorobenzene acetic acid as the starting material, through esterification, reduction, oxidation and Witting reaction, to obtain 4 - (2, 4, 5 - trifluorophenyl) - 2 - butene ethyl ester, or passes through the reduction, oxidation and Witting reaction after, to obtain 4 - (2, 4, 5 - trifluorophenyl) - 2 - butene ethyl ester. Then in BuLi or six methyl two silicon and nitrogen under the action of the alkane-sodium, with chiral amine on the hydroamination reaction, framed asymmetric amination product, through ester, condensation, hydrogenated three-step reaction to obtain sitagliptin. The west he of the spit of fland synthesis method of raw materials are cheap and easy to obtain, steps are less, the operation is easy, can be effectively reduced. The method can be the high purity of the sitagliptin, the salt of the phosphoric acid obtained after HPLC purity and sitagliptin ee values are in 99% or more, can be applied to the medical field. (by machine translation)
PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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Paragraph 0115, (2015/09/22)
The disclosure generally relates to compounds of formula I, II, III and IV, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.