- Improved syntheses of N-desmethylcitalopram and N,N-didesmethylcitalopram
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An improved and efficient synthesis of N-desmethylcitalopram (2) and N,N-didesmethylcitalopram (3) is presented. The method involved N-demethylation of citalopram (1) using 1-chloroethyl chloroformate to give 2 in 87% yield. Synthesis of 3 was accomplished by alkylation of 8 with 1-(3-bromopropyl)-2,2,5, 5-tetramethyl-1-aza-2,5-disilacyclopentane (9). Copyright Taylor & Francis Group, LLC.
- Jin, Chunyang,Boldt, Karl G.,Rehder, Kenneth S.,Brine, George A.
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p. 901 - 908
(2007/10/03)
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- Treatment or prophylaxis of migraine or headache disorders using citalopram, escitalopram or citalopram metabolites
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Methods for prophylaxis of or treating or preventing migraine or migraine headaches, or other headache disorders include administering to a subject in need of treatment a therapeutically effective amount of citalopram, escitalopram, or a racemic or optically pure citalopram metabolite, or pharmaceutically acceptable salts, solvates, polymorphs, or hydrates thereof.
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Page/Page column 11
(2010/02/13)
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- PREPARATION OF ESCITALOPRAM
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Enantiomerically enriched citalopram is prepared by methylating enantiomerically enriched didesmethylcitalopram, obtained by directly resolving racemic didesmethylcitalopram using a chiral acid.
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Page/Page column 26-27
(2008/06/13)
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- Method for the preparation of citalopram
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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.
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