Novel and Efficient Synthesis of Deuterium-Labeled Olopatadine-d6

Abstract

A novel and highly efficient synthetic approach has been developed for the synthesis of deuterium-labeled olopatadine-d₆ using inexpensive and commercially available dimethyl sulfate-d₆ at the stage of alkylation of primary amine intermediate. The proposed synthetic path makes it possible to avoid the use of expensive labeled reagents such as dimethyl amine-d₆ used as labeled precursor in the traditional synthetic route. The structure of the obtained olapatadine-d₆ has been confirmed by ¹H NMR and mass spectral data.