150322-73-9Relevant articles and documents
OXIDATIVE COUPLING OF ARYL BORON REAGENTS WITH SP3-CARBON NUCLEOPHILES, AND AMBIENT DECARBOXYLATIVE ARYLATION OF MALONATE HALF-ESTERS VIA OXIDATIVE CATALYSIS
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Paragraph 0724; 0725, (2018/07/29)
Described herein are methods of oxidative coupling of aryl boron reagents with sp3-carbon nucleophiles, and ambient decarboxylative arylation of malonate half-esters via oxidative catalysis.
PROCESS FOR THE PREPARATION OF HIGH-PURITY PRASUGREL
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Page/Page column 12, (2018/04/11)
The field of invention relates to a novel process, suitable for industrial scale manufacture, for the preparation of high-purity 5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4,5,6,7- tetrahydrothieno[3,2-c]pyridine-2-yl acetate, prasugrel, of Formula (I). Especially in large-scale production, one of the main causes of piling up the impurities is the use of ether solvents consequently in each step in this procedure ethers are excluded. Avoiding the ethers resulted new conditions for production of intermediates in the different steps of our procedure. Conditions were determined so that each step from the beginning contributes to minimizing the impurity content of the end-product.
Method for preparing antithrombotic drug prasugrel intermediate
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Paragraph 0025; 0047-0049, (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.