Method for obtaining a pharmaceutically active compound,...

Details Method for obtaining a pharmaceutically active compound,... Method for obtaining a pharmaceutically active compound,...

2006-06-26

2010-06-29

Seaman, D. Margaret (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C546S094000

Reexamination Certificate

active

07745628

ABSTRACT:
The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.

REFERENCES:
patent: 5561149 (1996-10-01), Azria et al.
patent: 87116119.6 (1988-05-01), None
patent: 89107764.6 (1989-11-01), None
patent: 2006056081 (2006-06-01), None
patent: WO 2006/056081 (2006-06-01), None

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