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:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="19" wi="65" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein R is hydrogen or loweralkyl,
<UnorderedLists id="ula01" listStyle="none"><ListItem>R' is lowealkyl,</ListItem><ListItem>R<Sup>2</Sup> is hydrogen, halo or loweralkoxy, Am is amino, methlamino or dimethylamino</ListItem></UnorderedLists>
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> |