PROCESS FOR THE PREPARATION OF AN INTERMEDIATE FOR A TRIAZOLOPYRIMIDINE CARBONUCLEOSIDE

摘要

A process for the preparation of 4,6-dihalopyrimidin-5-amines of formula (II), or salts thereof, which comprises reacting 5-aminopyrimidin-4,6-diols of formula (III), or salts thereof, or a solvate either of the compound of formula (III) or of a salt thereof, with a halogenating agent, new intermediates useful in the preparation of the compound of formula (II) and processes for the preparation of these intermediates. The invention also refers to a process for the preparation of ticagrelor or a pharmaceutically acceptable salt thereof from 4,6-dihalo-2-(propylthio)pyrimidin-5-amine of formula (IIA).

主权项

1. A process for the preparation of a compound of formula (II) or a salt thereof,wherein X is a halogen selected from the group consisting of chlorine, bromine and iodine; R is selected from the group consisting of H, SR′, NHR′, N(R′)2, CH3, CH2R′, CH(R′)2, and C(R′)3; and each R′ is independently selected from the group consisting of (C1-C5)alkyl, aryl, and (C1-C5)alkylaryl; which comprises reacting a compound of formula (III) or a salt thereof, or a solvate either of the compound of formula (III) or of a salt thereof,with a halogenating agent at a temperature comprised from 70 to 140° C.