Process for the preparation of midodrine,...

Details Process for the preparation of midodrine,... Process for the preparation of midodrine,...

C - Chemistry, Metallurgy

07

C

C07C 231/14 (2006.01) C07C 231/02 (2006.01) C07C 237/08 (2006.01)

Patent

CA 2421550

The present invention provides for a novel process for the preparation of Midodrine or a pharmaceutically acceptable salt thereof comprising: (a) a step of reacting 2-amino-1-(2',5'-dimethoxyphenyl) ethanol of formula 1 with an N-protected glycine of formula 2 containing an amino protecting group in the presence of 1,1'-carbonyldiimidazole (CDI); and (b) removing the amino protecting group by deprotection Image wherein R1 is a benzyl, triphenylmethyl, tert-butyloxycarbonyl, or a benzyloxycarbonyl group. This results in an unexpectedly efficient and cost-effective process. Additionally, the process is simple and safe as all the intermediates and reagents involved in the process pose no safety risks. Further reaction of Midodrine with a pharmaceutically acceptable acid affords a pharmaceutically acceptable salt thereof. Preferably, the pharmaceutically acceptable salt obtained from the process according to the present invention is Midodrine Hydrochloride.

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