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filingDate 2019-05-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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publicationDate 2020-05-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-111171002-A
titleOfInvention A kind of preparation method of PARP inhibitor intermediate
abstract The present invention relates to a kind of PARP inhibitor, especially the intermediate (R)-2-(1-(2-(tert-butyloxy)-2-oxoethyl)-2-methylpyrrolidine- of Pamiparib 2 base)-6-fluorine-1-toluenesulfonyl-1H-indole-4-The preparation method of methyl carboxylate, described method in the case of using palladium (Pd) catalyst and cuprous iodide (Cul) The palladium catalyst contains at least one or both of Pd(dppf)Cl2 and Pd(dtbpf)Cl2. The method can improve the conversion rate of raw materials and obtain products with high chiral purity. The method has stable production, good repeatability and high yield, and saves production costs in industrial large-scale production.
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