Process for synthesis of 1-(aminomethyl)cyclohexane acetic...

Details Process for synthesis of 1-(aminomethyl)cyclohexane acetic... Process for synthesis of 1-(aminomethyl)cyclohexane acetic...

2005-01-25

2005-01-25

Killos, Paul J. (Department: 1625)

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

Organic compounds

Carboxylic acids and salts thereof

Reexamination Certificate

active

06846950

ABSTRACT:
A process for synthesis of 1-(aminomethyl)cyclohexane acetic acid hydrochloride (Gabapentin hydrochloride) comprising:a) Reaction of a mixture of acetic anhydride/ammonium acetate with 1,1-cyclohexane-diacetic acid to yield 3,3-pentamethylene glutarimide;b) Treatment of 3,3-pentamethylene glutarimide with sodium hydroxide in an aqueous solution up to dissolution, dripping the solution thus obtained into a sodium hydroxide/sodium hypochlorite mixture, which is also aqueous, followed by acidification with hydrochloric acid to yield gabapentine hydrochloride.

REFERENCES:
patent: 4024175 (1977-05-01), Satzinger et al.
patent: 4152326 (1979-05-01), Hartenstein et al.
patent: 5091567 (1992-02-01), Geibel et al.
patent: 5362883 (1994-11-01), Jennings et al.
patent: 6054482 (2000-04-01), Augart et al.
Abstract of US Patent: 5132451.
Abstract of US Patent: 5095158.
Abstract: Gabapentin—Drugs of the Future vol. 9. No. 6 1984.
Abstract of US Patent: 5068413.
Abstract of US Patent: WO 9828255.

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