1176895-65-0Relevant articles and documents
Preparation method of 1-morpholinyl-4-(2,4,5-trifluorophenyl)butane-1,3-dione
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Paragraph 0082-0084, (2020/05/02)
The invention discloses a preparation method of 1-morpholinyl-4-(2,4,5-trifluorophenyl)butane-1,3-dione, and belongs to the technical field of organic synthesis. The preparation method comprises the following step: under the action of a metal chelating agent and an alkali, carrying out a reaction of the following formula on a compound 2 and a compound 3 in an organic solvent to obtain a compound 1. The preparation method disclosed by the invention is high in yield, simple in post-treatment, simple, feasible, mild in reaction condition and suitable for industrial production.
Phosphonic acid analogs of fluorophenylalanines as inhibitors of human and porcine aminopeptidases N: Validation of the importance of the substitution of the aromatic ring
Dziuk, B?a?ej,Kafarski, Pawe?,Pirat, Jean-Luc,Talma, Micha?,Wanat, Weronika
, (2020/05/04)
A library of phosphonic acid analogs of phenylalanine substituted with fluorine, chlorine and trifluoromethyl moieties on the aromatic ring was synthesized and evaluated for inhibitory activity against human (hAPN) and porcine (pAPN) aminopeptidases. Fluorogenic screening indicated that these analogs are micromolar or submicromolar inhibitors, both enzymes being more active against hAPN. In order to better understand the mode of the action of the most active compounds, molecular modeling was used. It confirmed that aminophosphonic portion of the enzyme is bound nearly identically in the case of all the studied compounds, whereas the difference in activity results from the placement of aromatic side chain of an inhibitor. Interestingly, both enantiomers of the individual compounds are usually bound quite similarly.
Preparation method of sitagliptin intermediate
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Paragraph 0034; 0035; 0036; 0037, (2017/11/18)
The invention belongs to the field of pharmaceutical synthesis, and particularly relates to a preparation method of a sitagliptin intermediate. The preparation method includes the steps of 1) acylating chlorination reaction: enabling 2,4,5-trifluorophenylacetic acid to directly react with sulfoxide chloride to generate a compound II; 2) Grignard reagent preparation: adding a compound III and magnesium chips, and triggering with iodine to obtain a Grignard reagent compound IV; 3) Grignard reaction: taking cuprous iodide as a catalyst, subjecting the compound II and the Grignard reagent compound IV to Grignard reaction to generate the sitagliptin intermediate-a compound V. The preparation method of the sitagliptin intermediate is simple in synthetic route, capable of producing highly-pure product, high in yield, low in cost, mild in reaction conditions, and applicable to industrialized production.