| 摘要 |
<p>Described is a process for the preparation of compounds of formula (1a) which comprises reacting an isomeric mixture consisting of from 75 to 95 % of compound of formula (2a) and from 5 to 25 % of a compound of formula (2b) with methylamine, in a suitable solvent, to form a sertraline imine isomeric mixture consisting of from 75 to 95 % of formula (1a) and from 5 to 25 % of formula (1b)(A1), or reacting an isomeric mixture consisting of from 75 to 95 % of a compound of formula (2a) and from 5 to 25 % of a compound of formula (2b) with methylamine, in a suitable solvent, using suitable methods of isolation to form an enriched sertraline imine isomeric mixture, consisting of gt; 99 % of a compound of formula (1a) and lt; 1 % of a compound of formula (1b)(A2); and then subjecting the sertraline imine isomeric mixture obtained according to reaction route (A1) or (A2), in a suitable solvent, to recrystallisation (B), in accordance with scheme (I) wherein in formula (1a), R1, R2 and R3 are each independently of the others hydrogen, halogen, trifluoromethyl or C1 C4alkoxy and formulae (1b), (2a) and (2b) are as defined in the description.</p> |
