发明授权
- 专利标题: METHOD FOR OBTAINING PIOGLITAZONE AS AN ANTIDIABETIC AGENT
- 专利标题(中): 用于生产吡格列酮糖尿病抗MITTTEL
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申请号: EP02734989.3申请日: 2002-04-25
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公开(公告)号: EP1387843B1公开(公告)日: 2007-02-28
- 发明人: HALAMA, Ales , HEJTMÁNKOVÁ, Ludmila , LUSTIG, Petr , RICHTER, Jindrich , SRSNOVÁ , Lucie , JIRMAN, Josef
- 申请人: Zentiva, a.s.
- 申请人地址: Dolni Mecholupy 130 102 37 Praha 10 CZ
- 专利权人: Zentiva, a.s.
- 当前专利权人: Zentiva, a.s.
- 当前专利权人地址: Dolni Mecholupy 130 102 37 Praha 10 CZ
- 代理机构: Jirotkova, Ivana
- 优先权: CZ20011501 20010426; CZ20011502 20010426
- 国际公布: WO2002088120 20021107
- 主分类号: C07D417/12
- IPC分类号: C07D417/12 ; A61K31/4427 ; A61P3/10
摘要:
A method for obtaining antidiabetic of formula (I), wherein the method comprises condensing of a 4-derivatized phenol or phenolate of general formula (II), wherein R is an amino group-containing organic residue, selected from the group comprising a residue of the following formula -NHR3, wherein R3 is hydrogen or a protecting group, which is removed before further treatment, and a residue of general formula (A), wherein Rb represents a carboxy group either in the free acid form or in the form of a salt or ester or another functional derivative or the nitrile group CN, and M represents a hydrogen or alkali metal atom, with a pyridine base of general formula (III), wherein Z is a leaving group other than a halogen, wherein, before or after carrying out the condensation, the following operations are carried out: (a) diazotizing the amino group present in organic residue R; (b) converting the diazotised residue R into a derivative of 2-halopropionate or 2-halopropionitrile of formula (B), wherein Rb is as defined above and X is a halogen; (c) cyclizing the derivative of 2-halopropionate or 2-halopropionitrile with thiourea; (d) hydrolysing the resulting imine thus giving pioglitazone of formula (I).
公开/授权文献
- EP1387843A1 METHOD FOR OBTAINING PIOGLITAZONE AS AN ANTIDIABETIC AGENT 公开/授权日:2004-02-11
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