发明名称 |
A METHOD FOR THE PREPARATION OF MIRTAZAPINE |
摘要 |
<p>The present invention relates to a method for the preparation of mirtazapine and tetracyclic analogous compounds having substantial enantiomeric excess of the R or S form. The invention further relates to a novel intermediate and its use for the preparation of mirtazapine having a substantial enantiomeric excess of the R or S form. The method comprising the steps of a: providing a carboxylic acid compound according to Formula (I) having a substantial enantiomeric excess of the R or S form, b: converting the carboxylic acid group of compound I into a ketone group, producing a ketone compound of Formula (II), c: optionally reducing ketone compound II with a mild reduction agent to form the intermediate hydroxy compound of Formula (III) and d: forming the mirtazapine of Formula (IV) by reduction of the ketone compound II or of the hydroxy compound III using a strong reduction agent.</p> |
申请公布号 |
WO2008125578(A3) |
申请公布日期 |
2008.12.24 |
申请号 |
WO2008EP54316 |
申请日期 |
2008.04.10 |
申请人 |
N.V. ORGANON;KEMPERMAN, GERARDUS JOHANNES |
发明人 |
KEMPERMAN, GERARDUS JOHANNES |
分类号 |
C07D471/14 |
主分类号 |
C07D471/14 |
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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