发明名称 |
PROCESS FOR THE SYNTHESIS OF ARFORMOTEROL |
摘要 |
<p>The present invention provides a process for preparing a compound of formula (Vl) 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 a-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 (Vl), 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.</p> |
申请公布号 |
CA2724882(A1) |
申请公布日期 |
2009.12.10 |
申请号 |
CA20092724882 |
申请日期 |
2009.06.02 |
申请人 |
CIPLA LIMITED |
发明人 |
HALDAVANEKAR, VAMAN VAISHALI;PRABHU, MANGESH;RAO, DHARMARAJ RAMACHANDRA;KANKAN, RAJENDRA NARAYANRAO |
分类号 |
C07C213/00;A61K31/167;A61P11/00;C07C213/08;C07C213/10;C07C217/86;C07C231/02;C07C233/43 |
主分类号 |
C07C213/00 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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