Synthetic Process of Rasagiline Mesylate

OBJECTIVE To optimize the synthetic process of rasagiline mesylate. METHODS First, 1-indanamine was synthesized from 1-indanone via reduction and amination. Then, R-(+)-N-propargyl-1-indanamine tartrate was obtained from 1-indanamine by condensation with 3-propargyl bromide, followed by resolution with L-tartaric acid. Finally, Rasagiline mesylate was prepared by alkalization and mesylation of the R-isomer L-tartrate. The total yield was 19.2%. RESULTS The chemical structures of intermediates and target product were confirmed by ¹H-NMR and MS. CONCLUSION This synthetic process is characterized by cheap materials, mild condition, simple operation and high yield, and is fitting for industrial application.