Preparation of citalopram used as antidepressant by dehydrating new oxazoline compound or thermally cleaving new thiazoline compound

摘要

Preparation (A) of citalopram comprises dehydrating new oxazoline compounds or thermally cleaving new thiazoline compounds. Preparation (A) of citalopram of formula (I) or its enantiomers or salts comprises treating an oxazoline compound of formula (IV) with a dehydration agent, or (when X = S), thermally cleaving the thiazoline ring, or treating in the presence of a radical initiator and optionally converting the free base or its acid addition salt to a salt. [Image] X : O or S; R 1>-R 3>H or 1-6C alkyl; R 4>H, 1-6C alkyl, carboxy or its precursor or CR 1>R 2> or CR 3>R 4>3-6C spiro-cycloalkane. Independent claims are included for the following: (1) new compounds of formula (VIII), (IX) and (IV) and (2) citalopram (I) prepared as above. [Image] ACTIVITY : Antidepressant. MECHANISM OF ACTION : None given.