62498-68-4Relevant academic research and scientific papers
PREPARATION OF ESCITALOPRAM
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Page/Page column 30-31, (2008/06/13)
Enantiomerically enriched citalopram is prepared by methylating enantiomerically enriched didesmethylcitalopram, obtained by directly resolving racemic didesmethylcitalopram using a chiral acid.
Method for the preparation of citalopram
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, (2008/06/13)
The invention relates to a method for the preparation of citalopram comprising reaction of a compound of formula II with a compound having the formula wherein R is halogen or —O—SO2-X, wherein X is alkyl, alkenyl, alkynyl or optionally alkyl substituted aryl or aralkyl, and R1 is dimethylamino, halogen, —O—SO2-X wherein X is as defined above, provided that R is not halogen when R1 is dimethylamino; and if R1 is dimethylamino followed by isolation of citalopram base or a pharmaceutically acceptable acid addition salt thereof, and if R1 is halogen or —O—SO2-X, wherein X is as defined above, followed by conversion of the resulting compound of formula wherein R2 is halogen or a group of formula —O—SO2-X wherein X is as defined above to citalopram, followed by isolation of citalopram base or a pharmaceutically acceptable acid addition salt thereof.
Method for the preparation of citalopram
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, (2008/06/13)
The present invention relates to a method for the preparation of citalopram comprising reaction a compound of formula (I) with a compound having the formula wherein X is a suitable leaving group and R is —CH2—O—Pg, —CH2—NPg1Pg2, —CH—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 Pg2 are protection groups for an amino group, R1 and R2 are independently selected from alkyl, alkenyl, alkynyl and optionally alkyl substituted aryl or aralkyl 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 and optionally alkyl substituted aryl or aralkyl and R8 is hydrogen or methyl; to form a compound of the formula 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.
