| 摘要 |
The present invention relates to a method for the preparation of citalopram comprising reaction a compound of formula (I) with a compound having formula (II) wherein X is a suitable leaving group and R is -CH2-O-Pg, -CH2-NPg1Pg2 , - CO-N(CH3)2, -CH(OR1)(OR2), -C(OR4)(OR5)(OR6), -COOR3, -CH2-CO-NH2, -CH=CHR7 and -CONHR8 wherein Pg is a protection group for an alcohol group, Pg1 and P g2 are protection groups for an amino group, R1 and R2 are independently select ed from alkyl, alkenyl, alkynyl and optionally alkyl substituted aryl or aralky l groups or R1 and R2 together form a chain of 2 to 4 carbon atoms, each of R3 , R4, R5, R6 and R7 are independently selected from alkyl, alkenyl, alkynyl an d optionally alkyl substituted aryl or aralkyl and R8 is hydrogen or methyl; t o form a compound of formula (III) wherein R is as defined above; followed by conversion of the group R to form a dimethylaminomethyl group and isolation of citalopram base or a pharmaceutically acceptable salt thereof.
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