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US 7,612,219 B2Granted
11—[ (Z) -3- (dimethylamino) propylidene]—6, 11-dihydro-dibenz [B,E] oxepin-2-YI ]—acetic acid
AssigneeUrquima, S.A.
InventorsJoan Bosch Cartés, Jordi Bachs Roca, Antonia Ma Gomez Gomez, Yolanda Alonso Marin, Mercè Bessa Sanchez
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Abstract
Process for the preparation of olopatadine (I), which comprises reacting a compound of formula (V) in the presence of a palladium catalyst to provide a compound of formula (VI), wherein the acid protecting group is removed to provide the compound of formula (I) and if desired, transformation into its salts.
Claims20
A process for the preparation of 11-[(Z)-3-(dimethylamino)propylidene]-6,11-dihydro-dibenz-[b,e]oxepin-2-yl acetic acid of formula 1 or a pharmaceutically acceptable salt thereof:
- comprising reacting a compound of formula V,
- wherein one of R1 and R2 is halogen and the other is CH═CH—CH2—CH2—N(CH3)2 and R3 is an acid protecting group, in the presence of a palladium catalyst, to obtain a compound of formula VI,
- and removing the acid protecting group R3 of said compound of formula VI to obtain the compound of formula I;
- and if desired, converting the compound of formula I into a pharmaceutically acceptable salt.
1 more element
Dependencies are inferred from the claim text.