Intermediates for the preparation of citalopram and...

Details Intermediates for the preparation of citalopram and... Intermediates for the preparation of citalopram and...

C - Chemistry, Metallurgy

07

D

C07D 307/88 (2006.01)

Patent

CA 2519629

Methods for manufacture of 5-alkoxycarbonylphthtalides are disclosed. The 5- alkoxycarbonylphthtalides are useful in syntheses of the well-known antidepressants citalopram and escitalopram. A method for preparing an alkoxycarbonylphtalide of formula (III) comprising: (a) reacting a compound of formula (VIIIa) with a formaldehyde and oleum; and (b) addition of an alcohol R3-OH to the reaction of step (a); wherein X and Y of formula (VIIIa) may be selected independently from the group consisting of: OR1, OR2, a halogen (such as C1, Br, I), and NR; wherein R, R1 and R2 are independently h or a C1-6- alkyl or phenyl.

Cette invention concerne des procédés de fabrication de 5-alcoxycarbonylphthalides. Ces 5-alcoxycarbonylphthalides sont utilisés dans des synthèses des antidépresseurs bien connus que sont le citalopram et l'escitalopram.

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