Process for preparing a piperidine derivative
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United States of America Patent
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Nov 9, 2004
Grant Date -
Jul 31, 2003
app pub date -
Jan 6, 2003
filing date -
Jun 13, 1996
priority date (Note) -
Expired
status (Latency Note)
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Abstract
A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R.sup.2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or --CO.sub.2 R.sup.7 group in which R.sup.7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R.sup.1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R.sup.2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R.sup.1 is hydrogen atom and Z is carbonyl group, then R.sup.2 is carboxyl group or --CO.sub.2 R.sup.7 group (R.sup.7 is as defined above); or (C) when R.sup.1 is hydrogen atom and Z is methylene group, then R.sup.2 is hydroxymethyl group.
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