Invention Grant
- Patent Title: Preparation method of ticagrelor and intermediates thereof
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Application No.: US14975785Application Date: 2015-12-20
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Publication No.: US09604991B2Publication Date: 2017-03-28
- Inventor: Xuenong Xu
- Applicant: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
- Applicant Address: CN Suzhou
- Assignee: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
- Current Assignee: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
- Current Assignee Address: CN Suzhou
- Agency: Perkins Coie LLP
- Priority: CN201310251364 20130624; CN201310258158 20130626; CN201310260749 20130627
- Main IPC: C07D471/00
- IPC: C07D471/00 ; C07D487/00 ; C07D491/00 ; C07D487/04 ; C07D317/44 ; C07D405/04

Abstract:
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 dialkyl carbonate (HI), to obtain 9-substituted-2,6-dihydroxy-8-azapurine (IV); chlorination of intermediate (IV), to obtain 9-substituted-2,6-dichloro-8-azapurine (V); an amination reaction of intermediate (V) and trans-(1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine (VI) generates 9-substituted-6-amino-substituted-2-chloro-8-azapurine (VII); and a propanethiolation reaction of intermediate (VII) and propanethiol (VIII), to obtain Ticagrelor (I). The preparation method is simple in process, has a high chemical and chiral purity and provides a new preparation method for industrializing Ticagrelor. In addition, also provided in the present invention are intermediates of Ticagrelor and a preparation method thereof, wherein raw materials of the preparation method are easily available, the conditions thereof are mild, and the yield thereof is high.
Public/Granted literature
- US20160102101A1 Preparation method of Ticagrelor and intermediates thereof Public/Granted day:2016-04-14
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