发明授权
- 专利标题: Process for the synthesis of arformoterol
- 专利标题(中): 合成阿霉素的方法
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申请号: US12995016申请日: 2009-06-02
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公开(公告)号: US09029421B2公开(公告)日: 2015-05-12
- 发明人: Vaishali Vaman Haldavanekar , Mangesh Prabhu , Dharmaraj Ramachandra Rao , Rajendra Narayanrao Kankan
- 申请人: Vaishali Vaman Haldavanekar , Mangesh Prabhu , Dharmaraj Ramachandra Rao , Rajendra Narayanrao Kankan
- 申请人地址: IN Mumbai
- 专利权人: Cipla Limited
- 当前专利权人: Cipla Limited
- 当前专利权人地址: IN Mumbai
- 代理机构: Conley Rose, P.C.
- 代理商 Rodney B. Carroll
- 优先权: IN1172/MUM/2008 20080602
- 国际申请: PCT/GB2009/001373 WO 20090602
- 国际公布: WO2009/147383 WO 20091210
- 主分类号: C07C217/86
- IPC分类号: C07C217/86 ; C07C213/02 ; C07C217/70 ; C07C213/00 ; C07C213/08 ; C07C213/10 ; C07C231/02 ; C07C233/43
摘要:
The present invention provides a process for preparing a compound of formula (VI) or a salt thereof, the process comprising: (i) reacting 4-methoxyphenyl acetone with an amine of formula (VIII) under conditions of reductive amination to produce a compound of formula (II) or a salt thereof, wherein there is no isolation of an imine intermediate formed during the reductive amination; (ii) condensing the compound (II) or the acid addition salt thereof with an α-haloketone of formula (III) to produce the compound of formula (IV); (iii) reducing the compound (IV) to a compound of formula (V); and (iv) reducing the compound (V) to the compound of formula (VI), wherein the reduction is carried out in the presence of either (1) a hydrogen donating compound in the presence of a hydrogen transfer catalyst; or (2) ammonium formate using a hydrogenation catalyst, wherein R1 and R2 are independently optionally substituted arylalkyl, and Hal is selected from chloro or bromo.
公开/授权文献
- US20110166237A1 Process for the Synthesis of Arformoterol 公开/授权日:2011-07-07
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