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http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-40
filingDate 2021-05-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_be8201bbc42b63b9c9e85d5c32c9f15c
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publicationDate 2022-10-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2022222203-A1
titleOfInvention Method for preparing trisubstituted indole compound by using one-step method
abstract Disclosed is a method for preparing a trisubstituted indole compound by using a one-step method. The present invention belongs to the technical field of pharmaceutical intermediate synthesis. In the present invention, the trisubstituted indole compound has a structure as represented by formula I, wherein R1 is alkyl, phenyl, benzyl, 2-isopropylphenyl or naphthyl; R2 is alkyl; R3 is alkyl, phenyl or a derivative thereof, and R4 is hydrogen, 4-methyl or 7-methyl/Cl/Br. The preparation method comprises the following steps: sequentially adding acetonitrile, 1-substituted indole and brominated sulfoxide imine; stirring and mixing to react thoroughly, and then stirring same at room temperature to react thoroughly; and performing column purification to finally obtain the indole trisubstituted compound. In the preparation method of the present invention, a highly-active trisubstituted indole is prepared by using a two-component reaction without additives and catalysts. The operation is simple, the reaction yield is high, and the product is easy to purify. The raw materials which are used are inexpensive and readily available. The reaction conditions are simple, mild and environmentally-friendly, have excellent substrate suitability, and obtain very high yields for most compounds.
priorityDate 2021-04-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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