Process for preparing 1S- 1 alpha, 2-alpha, 3-beta (1S *, 2R *), 5-beta - 3- 7- 2- (3,4-difluorophenyl) -ciclopropilamino -5- (propylthio) -3H-1,2,3-triazolo 4,5-d pyrimidin-3-yl -5- (2-hydroxyethoxy) cyclopentane-1,2-diol and their intermediates

摘要

Process for preparing a compound of formula (I) ** ** Formula comprising (a) reacting a compound of formula (II) ** ** Formula with oxalic acid to form the oxalate salt of the compound of formula (II) wherein it is carried out the reaction in ethanol or a mixture of water and ethanol after which ethyl iso -propyl the reaction mixture is added; and (b) reacting the salt of the compound of formula (II) with an excess of a compound of formula (VI) ** ** Formula in the presence of triethylamine at between 80 ° and 115 ° C at an oxygen concentration below 0, 5% by volume, to obtain the compound of formula (III) ** ** formula and isolating the compound of formula (III) in crystalline form; c) reacting the compound of formula (III) with acetic acid and sodium nitrite at between 20 and 30 to obtain the compound of formula (IV) ** ** Formula and (d) reacting the compound of formula 5 (IV ) with a compound of formula (VII) at a temperature equal to or below 40 ** ** formula in which is added the compound of formula (VII) is added to the reaction mixture in step (d) to a rate that maintains the reaction temperature at or below 30 ° C, to obtain the compound of formula (V) ** ** formula and (e) deprotecting the compound of formula (V) using aqueous hydrochloric acid in methanol in a biphasic system for obtain the compound of formula (I).