Invention Grant
- Patent Title: Method for preparing aliskiren and its intermediates thereof
- Patent Title (中): 阿利吉仑及其中间体的制备方法
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Application No.: US13639144Application Date: 2010-04-19
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Publication No.: US08664440B2Publication Date: 2014-03-04
- Inventor: Yongjun Tu , Yi Zhang , Rongde Cheng , Lingchao Peng
- Applicant: Yongjun Tu , Yi Zhang , Rongde Cheng , Lingchao Peng
- Applicant Address: CN Taizhou
- Assignee: Zhejiang Tianyu Pharmaceutical Co., Ltd
- Current Assignee: Zhejiang Tianyu Pharmaceutical Co., Ltd
- Current Assignee Address: CN Taizhou
- Agency: Stites & Harbison PLLC
- Agent Cong Ding
- Priority: CN201010000057 20100106
- International Application: PCT/CN2010/000526 WO 20100419
- International Announcement: WO2011/082506 WO 20110714
- Main IPC: A61K31/16
- IPC: A61K31/16 ; C07C239/00

Abstract:
A method for preparing Aliskiren and intermediate thereof, which comprises the following steps: reacting 4-bromo-1-methoxy-2-(3-methoxypropoxy)benzene with magnesium isopropyl chloride and n-BuLi to obtain the compound of formula XXII; reacting the product of methylsulfonylation of the compound of formula XIX with anhydrous LiBr to obtain the compound of formula XXI; obtaining the intermediate of Aliskiren shown as formula XV by reacting the compound of formula XXII with the compound of formula XXI in an ether as the solvent and in the presence of a catalyst containing iron; then reacting the compound of formula XV with the compound of formula VII to obtain the compound of formula XXIII, following removing R1 from the amino group and obtaining Aliskiren shown as formula I.
Public/Granted literature
- US20130225841A1 METHOD FOR PREPARING ALISKIREN AND ITS INTERMEDIATES THEREOF Public/Granted day:2013-08-29
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