http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2643811-C2

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publicationDate 2018-02-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2643811-C2
titleOfInvention Method for production of hydroxylated cyclopentyl pyrimidine compounds
abstract FIELD: pharmacology. n SUBSTANCE: compounds of formula I can be used to prepare compounds possessing the properties of an ACT kinase inhibitor for treatment of diseases such as cancer. The method for preparation of a compound of formula I comprises cyclising of a compound of formula II or a salt thereof, wherein R 1 is t-butoxycarbonyl; R 2 is -COOR a , where R a is hydrogen or unsubstituted C 1-4 alkyl, or R 2 is-CONR a R b , where R a is unsubstituted C 1-4 alkyl and R b is -OR c , phenyl; or R a and R b are taken together with the atom to which they are attached to form a 5-7 membered heterocyclyl, further comprising an oxygen atom; R c is C 1-4 alkyl; and M is Li or Mg. At that, a compound of formula II or a salt thereof obtained by contacting of a compound of formula III or a salt thereof, wherein R 3 is bromine or iodine, with a magnesium or lithium metal-containing agent, for example alkyl magnesium halide, is used. The compound of formula III is usually prepared by reacting a compound of formula IV or a salt thereof with compound to produce a compound of formula V or a salt thereof, wherein R 4 is -Cl or -OH, R 1 and R 2 have the values indicated above. The invention also relates to new intermediates, a compound of formula III and a compound of formula IV. n EFFECT: method allows to obtain products on an industrial scale with comparable or increased yield and quality of products. n 22 cl, 1 tbl, 6 ex n ,
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