| 摘要 |
<p>Disclosed in the present invention is a method for preparing Ticagrelor (I), comprising the following steps: a cyclization reaction of 5-amino-1,4-di-substituted-1,2,3-triazole (II) and a sulphur-containing cyclization agent (III), to obtain 9-substituted-2-sulpho-6-oxo-8-azapurine (IV); a substitution reaction of intermediate (IV) and halopropane (V) generates 9-substituted-2-propanethiol-6-oxo-8-azapurine (VI); chlorination of intermediate (VI) and an amination reaction of intermediate (VI) and trans-(1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine (VII) generates 9-substituted-6-amino-substituted-2-propanethiol-8-azapurine (VIII); and intermediate (VIII) removes the methylene acetone protecting group to obtain Ticagrelor (I). The preparation method is simple in process, economic and environmentally friendly, has a high chemical and chiral purity and provides a new preparation method for the industrial production of Ticagrelor.</p> |
