Method for the preparation of citalopram
AssigneeH. Lundbeck A.S.
InventorHans Petersen
Life of this patent
Estimating the term…
Abstract
The invention relates to a method for the preparation of citalopram comprising, in either order, subjecting a compound of formula wherein Y is a cyano group or a group which may be converted to a cyano group, R is hydrogen, —O—R1, NH2, NHCH3 or —N(CH3)2 wherein R1 is selected from hydrogen, alkyl, alkenyl, alkynyl and optionally alkyl substituted aryl or aralkyl; to i) reduction of the double bond in the side chain of formula —CH═CH—COR: ii) conversion of the group—COR or a reduced form thereof to a dimethylaminomethyl group; and iii) if Y is not cyano, conversion of the group Y to a cyano group; followed by isolation of citalopram base or a pharmaceutically acceptable acid addition salt thereof.
Claims10
A method for the preparation of citalopram comprising subjecting, in either order, a compound of formula
- wherein Y is a cyano group or a group which may be converted to a cyano group, R is hydrogen, —O—R1, NH2, NHCH3 or —N(CH3)2 wherein R1 is selected from hydrogen, alkyl, alkenyl, alkynyl and optionally alkyl substituted aryl or aralkyl;
- to
- i) reduction of the double bond in the side chain of formula —CH═CH—COR;
- ii) conversion of the group —COR or a reduced form thereof to a dimethylaminomethyl group;
- and
- iii) if Y is not cyano, conversion of the group Y to a cyano group;
- followed by isolating citalopram base or a pharmaceutically acceptable acid addition salt thereof.
A compound having the formula
- wherein Y is a cyano group or a group which can be converted to a cyano group, R is hydrogen, —O—R1, NH2, NHCH3 or —N(CH3)2 wherein R1 is selected from hydrogen, alkyl, alkenyl, alkynyl and optionally alkyl substituted aryl or aralkyl, or an acid addition salt thereof.
Dependencies are inferred from the claim text.