发明名称 Process for the preparation of 2-alkoxy-N-(1-azabicyclo[2.2.2]octan-3-yl) aminobenzamides.
摘要 <p>A process for the preparation of 2-alkoxy- N-(1-azabicyclo[2.2.2]octan-3-yl) aminobenzamides, which are gastric pharmaceuticals in monogastric animals having the formaula: &lt;Chemistry id="chema01" num="0001"&gt;&lt;Image id="ia01" he="19" wi="65" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;wherein R is hydrogen or loweralkyl, &lt;UnorderedLists id="ula01" listStyle="none"&gt;&lt;ListItem&gt;R' is lowealkyl,&lt;/ListItem&gt;&lt;ListItem&gt;R&lt;Sup&gt;2&lt;/Sup&gt; is hydrogen, halo or loweralkoxy, Am is amino, methlamino or dimethylamino&lt;/ListItem&gt;&lt;/UnorderedLists&gt; is disclosed wherein in the initial step an appropriate monoprotonated 3-aminoquinuclidine strong acid salt and an appropriate amino benzoic acid all in a 50-90 vol. % pyridine in water solution are reacted in the presence of N,N'-dialkylcarbodiimide. The free base may be obtained by conventional procedures from the mixtures with minimal purification effort.</p>
申请公布号 EP0190915(A2) 申请公布日期 1986.08.13
申请号 EP19860300728 申请日期 1986.02.04
申请人 A.H. ROBINS COMPANY, INCORPORATED 发明人 LO, YOUNG SEK
分类号 C07D453/02 主分类号 C07D453/02
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