CRYSTALLINE SINGLE DIASTEREOMERS OF 2-CYANO-3-ARYLGLUTARATE ESTERS

摘要

For preparing the pharmaceutically active compound paroxetine and intermediates therefor, crystalline 2-cyano-3-(4'-fluorophenyl)glutarates are obtained as a single diastereomer and reduced to give a trans-piperidinone, which is conventionally worked up to paroxetine. Paroxetine is the (-) trans isomer of 4-(4'-fluorophenyl)-3-(3',4'-methylenedioxyphenoxymethyl)-piperidine and is used in therapy as the hydrochloride salt to treat inter alia depression, obsessive compulsive disorder (OCD) and panic.