204205-33-4Relevant articles and documents
2 - Bromo 2 - (2 - fluorophenyl) ethanone preparation of cyclopropyl (by machine translation)
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Paragraph 0040; 0044; 0047; 0048; 0052; 0056, (2018/04/26)
The invention belongs to the technical field of medicines and particularly relates to a preparation method of a medicine intermediate, and more particularly relates to a preparation method of a prasugrel intermediate cyclopropyl-2-bromo-2-(2-fluorophenyl) ethanone. The preparation method comprises the following steps: carrying out reaction on 2-fluorophenylacetate and cyclopropane carbonyl chloride to prepare cyclopropyl-2-(2-fluorophenyl) ethanone; and then, carrying out halogenating reaction with a bromination reagent to prepare cyclopropyl-2-bromo-2-(2-fluorophenyl) ethanone. The preparation method provided by the invention is carried out under a relatively mild condition, raw materials are easily available, and the obtained product is high in purity and relatively high in yield which reaches over 70%, so that the preparation method is suitable for industrial production.
Method for preparing antithrombotic drug prasugrel intermediate
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, (2017/04/03)
The invention discloses a method for preparing an antithrombotic drug prasugrel intermediate. The method includes the following steps that firstly, fluorobenzene makes contact and reacts with 1-bromine-3-alkene-diacetyl to generate 1-(2-fluoro-phenyl)-3-alkene-diacetyl under catalysis of Lewis acid, wherein Lewis acid is stannic chloride; secondly, 1-(2-fluoro-phenyl)-3-alkene-diacetyl generated by 1-bromine-3-alkene-diacetyl reacts with dimethyl phosphite methyl sulfonium or dimethyl sulfoxonium methylide to generate 1-cyclopropyl-2-(2-fluoro-phenyl)-2-ethanone; thirdly, 1-cyclopropyl-2-(2-fluoro-phenyl)-2-ethanone obtained in the second step reacts with a bromide reagent to generate the prasugrel intermediate, namely 1-cyclopropyl-2 bromine-2-(2-fluoro-phenyl)-2-ethanone. A brand-new technology is provided for the prasugrel intermediate and synthesis of the prasugrel intermediate, cost is low, the yield is high, processing is easy, and the method is suitable for industrial production.
IMPROVED PROCESS FOR THE PREPARATION OF PRASUGREL AND INTERMEDIATE THEREOF
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Page/Page column 16, (2014/08/07)
The invention relates to an industrial scale process for the preparation of l-cyclopropyl-2-(2- fluorophenyl)-ethanone of the Formula (1) and the use of this compound for the preparation of prasugrel.