Potassium Carbonate → Rasagiline

Participants

Reaction Steps

Another process for preparation of Rasagiline hydrochloride as disclosed in EP '492 comprises reaction of R(−)-1-aminoindan (8) with propargyl chloride (6) in presence of potassium carbonate in acetonitrile (ACN) at 60° C. for 16 hours to obtain R(+) Rasagiline base (9) which is then purified by column chromatography. The purified base is then converted to R(+)-Rasagiline hydrochloride followed by recrystallization with isopropanol. The main disadvantage of this process is longer reaction time (16 hours) and low overall yield of about 56%.

Provenance & Evidence