发明名称 |
METHOD FOR OBTAINING PIOGLITAZONE AS AN ANTIDIABETIC AGENT |
摘要 |
<p>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 -NHR<3>, wherein R<3> is hydrogen or a protecting group, which is removed before further treatment, and a residue of general formula (A), wherein R<b> 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 R<b> 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).</p> |
申请公布号 |
WO02088120(A1) |
申请公布日期 |
2002.11.07 |
申请号 |
WO2002CZ00024 |
申请日期 |
2002.04.25 |
申请人 |
LECIVA, A.S.;HALAMA, ALES;HEJTMANKOVA, LUDMILA;LUSTIG, PETR;RICHTER, JINDRICH;SRSNOVA, LUCIE;JIRMAN, JOSEF |
发明人 |
HALAMA, ALES;HEJTMANKOVA, LUDMILA;LUSTIG, PETR;RICHTER, JINDRICH;SRSNOVA, LUCIE;JIRMAN, JOSEF |
分类号 |
A61K31/4427;A61P3/10;C07D417/12;(IPC1-7):C07D417/12;A61K31/442 |
主分类号 |
A61K31/4427 |
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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