Process for the preparation of 2- (2- (4- (bis (4-flourophenyl) methyl) -pipe razin-1-yl) ethoxy acetic acid derivatives or corresponding salt forms thereof and intermediates therefor
OwnerOusmane Diouf, John Surteesinventors
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Abstract
The present invention relates to a process for the manufacture of 2-{2-[4-(bis(4-fluorophenyl)methyl)-1-piperazinyl]ethoxy}acetic acids, amides or related derivatives, of the general formula (I) wherein: Y represents hydroxy or —NR1R2; R1 and R2 each independently represent hydrogen or C?1-4#191 alkyl; m is 1 or 2, and n is 1 or 2, as well as the non-toxic, pharmaceutically acceptable salts and mixtures thereof. The present invention concerns also a polymorphic form of efletirizine.
Claims15
1-23. (canceled)
A process for the manufacture of 2-(2-(4-(bis(4-fluorophenyl)methyl)-1-piperazinyl)ethoxy)acetic acids, amides and related derivatives of the general formula (I)
- wherein:
- Y represents hydroxy, or —NR1R2;
- R1 and R2 each independently represent hydrogen or C1-4 alkyl;
- m is 1 or 2, and n is 1 or 2, as well as non-toxic, pharmaceutically acceptable salts, and mixtures thereof which comprises
- a) reacting compound of formula (II)
- wherein L1 represents a leaving group with a compound of formula (III)
- wherein n and m are defined as above, in the presence of a base and an inert solvent, and
- b) reacting the corresponding compound of formula (IV) thus obtained
- with a compound of formula (V)
- wherein L2 represents a leaving group and Y is defined as above, in the presence of an inert solvent and a proton acceptor.
Dependencies are inferred from the claim text.