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US 2004/0073038 A1Published application
Process of preparing paroxetine and intermediates for use therein
OwnerGeorge Leo Callewaertinventor
Life of this patent
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Abstract
A process of preparing paroxetine, a process for preparing intermediates for use in the preparation of paroxetine and specific intermediates useful in paroxetine preparation. The specific intermediates that can be employed include compounds of formulae (V), (VI), or (VII). 1
Claims57
A process of preparing a compound of formula (V)
- 21
- from a compound of formula (VII)
- 22
- where
- R3 represents hydrogen or halo;
- R4 represents —C(═O)OR7where R7 represents optionally substituted alkyl or aralkyl;
- R5 represents optionally substituted alkyl, alkoxyalkyl, aralkyl or (heterocycle)alkyl;
- and
- R6 represents —C(═O)NHR5, where R5 is as defined above.
6 more elements
A process of preparing a compound of formula (V)
- 24
- from a compound of formula (VI)
- 25
- where
- R3 represents hydrogen or halo;
- R4 represents —C(═O)OR71, where R7 represents optionally substituted alkyl or aralkyl;
- R5 represents optionally substituted alkyl, alkoxyalkyl, aralkyl or (heterocycle)alkyl;
- and
- R6 represents —C(═O)NHR5, where R5 is as defined above.
6 more elements
A compound of formula (Vb), and salts thereof
- 28
- where
- R3 represents hydrogen or halo;
- R4b represents —C(═O)OR4a, where R4a is selected from the group consisting of 2-bromoethyl, 2,2,2-trichloroethyl, 2,2,2-trichloro-1,1-dimethylethyl and t-butyl, 2-ethylhexyl and benzyl;
- and
- R5 represents optionally substituted alkyl, alkoxyalkyl, aralkyl or (heterocycle)alkyl.
3 more elements
29 30 31
A compound of formula (VII), and salts thereof
- 32
- where
- R3 represents hydrogen or halo;
- R5 represents optionally substituted alkyl, alkoxyalkyl, aralkyl or (heterocycle)alkyl;
- and
- R6 represents —C(═O)NHR5, where R5 is as defined above.
3 more elements
33
A compound of formula (VI)
- 34
- where
- R3 represents hydrogen or halo;
- R4 represents —C(═O)OR7, where R7 represents optionally substituted alkyl or aralkyl;
- R5 represents optionally substituted alkyl, alkoxyalkyl, arallkyl or (heterocycle)alkyl;
- and
- R6 represents —C(═O)NHR5, where R5 is as defined above.
4 more elements
35 36
Dependencies are inferred from the claim text.