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filingDate 2011-03-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2013-06-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-2013523605-A
titleOfInvention Sitagliptin intermediate, preparation method and use thereof
abstract The present invention relates to a compound of formula (f) which is a sitagliptin intermediate, a process for its preparation and its use. The compound of formula (f) is prepared by reacting the compound of formula (a) with an electrophilic substitution reaction with benzyl halide and reacting the compound of formula (b) with the compound of formula (i). A new compound of formula (e) is obtained, and a Grignard reagent obtained from 2,4,5-trifluorobromobenzene and magnesium is reacted with the compound of formula (e) to form a new compound. In this method, a compound of the formula (f) is obtained, and the compound of the formula (f) is a new intermediate compound for synthesizing the sitagliptin intermediate (g). The compound of the formula (f) is reduced by palladium carbon, and the compound of the formula (g) is obtained by removing the benzyl group and attaching a protecting group. The structural formula of the compound according to the present invention is as follows, wherein R is a protecting group for a carboxyl group, and R 2 is a (substituted) hydrocarbon group.
priorityDate 2010-03-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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