875050-51-4Relevant articles and documents
Stereoselective syntheses of the antihistaminic drug olopatadine and its E-isomer
Bosch, Joan,Bachs, Jordi,Gomez, Antonia M.,Griera, Rosa,Ecija, Marta,Amat, Mercedes
experimental part, p. 6340 - 6344 (2012/10/07)
Practical stereoselective synthetic routes to the antihistaminic drug olopatadine and its E-isomer have been developed, the key steps being a trans stereoselective Wittig olefination using a nonstabilized phosphorus ylide and a stereoselective Heck cyclization. The stereoselectivity of the Wittig reaction depends on both the phosphonium salt anion and the cation present in the base used to generate the ylide.
PROCESS FOR THE PREPARATION OF 11-[(Z)-3-(DIMETHYLAMINO)PROPYLIDENE]-6,11-DIHYDRO-DIBENZ[B,E]OXEPIN-2-YL]-ACETIC ACID
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Page/Page column 12, (2008/06/13)
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.