New H <sub> 1 </ Sub> Receptor Antagonist Criolo He Will Synthesis Process Research

Olopatadine Hydrochloride, a new H₁ receptor antagonist, was approved to go to the market in USA in 1997. It is considered to have a high affinity for histamine H₁ receptor and no effect on alpha-adrenergic and serotonin receptors.In this thesis the synthetic method of Olopatadine Hydrochloride was studied. Olopatadine was synthesized by six steps. The yield of the Wittig reaction was raised from 61% to 78%. The separate method of E/Z isomers was simplified. The total yield of the six-step reaction was also raised from 7.3% to 11.3%.The structure of target molecule was determined by IR, ¹³C-NMR, ¹H-NMR and MS spectrum.