发明名称 Process for the preparation of indolinone-2 derivatives.
摘要 <p>A process for the preparation of a compound of structure (I) &lt;CHEM&gt; in which, each group R is hydrogen, C1-6alkyl, C3-6allyl, phenylC1-6alkyl or 4-hydroxyphenylC1-6alkyl; R&lt;1&gt;, R&lt;2&gt; and R&lt;3&gt; are hydrogen or C1-6alkyl; R&lt;4&gt; is hydrogen or hydroxy: and n is 1 to 3 or a pharmaceutically acceptable salt thereof, which comprises reduction of a compound of structure (II) &lt;CHEM&gt; in which R, R&lt;2&gt; to R&lt;4&gt; and n are as described above and R&lt;5&gt; is hydrogen or a cation, followed by cyclisation of the intermediate so formed, and, optionally, alkylating to form a compound of structure (I) in which R&lt;1&gt; is C1-6alkyl and, optionally, forming a pharmaceutically acceptable salt thereof, characterised in that the reduction of the compound of structure (II) is carried out by catalytic transfer hydrogenation in water as a solvent.</p>
申请公布号 EP0266033(A2) 申请公布日期 1988.05.04
申请号 EP19870307510 申请日期 1987.08.25
申请人 SMITH KLINE & FRENCH LABORATORIES LIMITED 发明人 WALSGROVE, TIMOTHY CHARLES;OXLEY, PAUL
分类号 B01J23/44;C07B61/00;C07D209/34;(IPC1-7):C07D209/34 主分类号 B01J23/44
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