Method for preparing ticagrelor solution

Abstract

The invention discloses a method for preparing a ticagrelor solution. According to the invention, hydroxy of a ticagrelor I crude product is protected by a protective group, then a crude product of a compound II is separated and purified to obtain the high purity compound II; the hydroxy protective group of the high purity compound II is removed under proper reaction conditions, a reaction mixture is post-processed and then the by-product is removed to obtain the high purity ticagrelor I, the ticagrelor I, a solvent or / and pharmaceutic adjuvant form a solution, after the solvent is removed, ticagrelor or a mixture containing ticagrelor and accessory with medicinal requirement can be obtained. The method has the advantages of mild reaction condition, simple operation, low cost, and environmental protection, and is suitable for industrial production.

Description

technical field

[0001] The invention relates to a purification method of an anticoagulant drug, in particular to a preparation method of a ticagrelor solution. Background technique

[0002] Ticagrelor, trade name Brilinta, chemical name: (1S,2S,3R,5S)-3-[7-{[(1R,2S)-2-(3,4 -Difluorophenyl)cyclopropyl]amino}-5-(propylthiouracil)-3H-[1,2,3]-triazolphos[4,5-d]pyrimidin-3-yl]-5 -(2-hydroxyethyl) cyclopentane-1,2-diol, its structure is as shown in formula (I):

[0003]

[0004] Ticagrelor (Ticagrelor) is a new type of platelet aggregation inhibitor developed by AstraZeneca, which is used for acute coronary syndrome (unstable angina, non-ST-segment elevation myocardial infarction or ST-segment elevation). Myocardial infarction) patients, including patients receiving drug therapy and percutaneous coronary intervention (PCI) to reduce the incidence of thrombotic cardiovascular events, was approved by the US Food and Drug Administration (FDA) in July 2011. Ticagrelor is a novel...

Images