| 摘要 |
<p>The invention relates to a process for the preparation of a compound of general formula (I)
<Chemistry id="chema01" num="0001"><Image id="ia01" he="24" wi="84" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein R<Sup>1</Sup> represents a hydrogen atom or a C<Sub>1-10</Sub> alkyl, C<Sub>3-7</Sub></p><p>cycloalkyl, C<Sub>3-7</Sub> cycloalkyl-(C<Sub>1-4</Sub>)alkyl, C<Sub>3-6</Sub> alkenyl, C<Sub>3-10</Sub> alkynyl, phenyl or phenyl-(C<Sub>1-3</Sub>alkyl group, and one of the groups represented by R<Sup>2</Sup>, R<Sup>3</Sup> and R<Sup>4</Sup> is a hydrogen atom or a C<Sub>1-6</Sub> alkyl, C<Sub>3-7</Sub> cycloalkyl, C<Sub>2-6</Sub> alkenyl or phenyl-(C<Sub>1-3</Sub>)alkyl group and each of the other two groups, which may be the same or different, represent a hydrogen atom or a C<Sub>1-6</Sub> alkyl group; or a salt or protected derivative thereof, by cyclisation of a compound of general formula (II)
<Chemistry id="chema02" num="0002"><Image id="ia02" he="28" wi="87" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein R', R<Sup>2</Sup>, R<Sup>3</Sup> and R<Sup>4 </Sup>are as defined above, or a salt or a protected derivative thereof.</p><p>The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.</p> |
