FORM 2
THE PATENT ACT 1970 (39 of 1970) & The Patents Rules, 2003 COMPLETE SPECIFICATION (See section 10 and rule 13)
1. TITLE OF THE INVENTION: "A process for preparation of Isonipecotamide"
2. APPLICANT (S)
(a) NAME: Centaur Pharmaceuticals Pvt. Ltd.
(b) NATIONALITY: An Indian Company incorporated under the Indian Companies ACT
1956
(c) ADDRESS: Centaur Pharmaceuticals Pvt. Ltd.
Centaur House, shanti Nagar,Vakola, Santacruz (e) Mumbai 400055. Tel No. 91-22-66499144 Fax No. 91-22-66499108/112
3. PREAMBLE TO THE DESCRIPTION
The following specification particularly describes the invention and the manner in which it is to be performed.

A process for preparation of isonipecotamide
The field of invention;
The field of invention relates to the process for preparation of isonipecotamide having formula I,

Background of the invention;
The compound of formula I is known as the isonipecotamide or 4-piperidinecarboxamide which is
used as an intermediate to form 4-piperidinecarboxamide derivatives used for the synthesis of 4-
piperidinecarboxamide derivatives useful as agents for improving the impaired brain function. 4-
piperidinecarboxamide is used for synthesis of derivatives such as N-[(2-oxo-l-pyrrolidinyl)-acetyl]-
peptide side chain at 1 position improve the impaired brain function, the same effective for
treatment of treatment of the impairment of memory by different causes such as multiple infracted
dementia, senile dementia, Alzheimer's dementia, sequel of cerebral injury and cerebral apoplexy
and the like, various agents such as cerebral vasodilators, agents for improving cerebral metabolism,
nootropic agents and the like have been proposed, but the satisfactory improvement could not be
obtained by any of these agents.
Object of the invention
It is an object of the invention is to provide a process for preparation of isopecotamide having formulal;


By catalytic hydrogenation of the isonicotinamide;
It is an object of the invention is to provide a process for preparation of isopecotamide having higher yield.
It is an object of the invention is to provide a process for preparation of isopecotamide which results in pure end product.
It is also an object of the invention is to provide a process for preparation of isopecotamide which yield harmless bi-product.
Detailed description of the Invention;
According to one of the aspect of the invention it is provided as catalytic hydrogenation process of isonicotinamide in presence of platinum group elements on carbon formed by reacting palladium with organochlorine, alcohol solvents at a temperature in the range of 25-50 °C isolate in s non-polar solvents.

The strength of the platinum group elements on carbon is in the range of 5-10 %, more particularly it is in at 10%.
According to the present invention the catalytic hydrogenation is carried out in presence of platinum group elements more preferably palladium and/or platinum.
In an another aspect of the invention organo-chlorine solvents used for the process is benzyl chloride, ethyl chloride, propyl chloride or combination thereof; and alcohols such as methanol, ethanol, propanol or combination thereof.

Also, non-polar solvents used in the catalytic hydrogenation process are Toluene, benzene, 1, 4-dioxane combination thereof.
In an another aspect of the invention the temperature of the catalytic hydrogenation process is in the range of 25-50 °C, more particularly the process is carried out at a temperature of 40-45 °C.
Example 1:
The isonicotinamide (50gm) was dissolved in methanol (450 ml).p-Chiorobenzyl chloride (52 gm) and 10% Palladium on Charcoal (5gm) slurry in Methanol (50ml) was added in autoclave reactor. Autoclave reactor was flushed with nitrogen twice and again flushed with hydrogen. Hydrogen gas was charged 6-8 kg at 40-45°C. Progress of reaction was monitored by thin layer chromatography. Reaction mixture was filtered and washed with methanol (300 ml). Methanol was distilled out and isonipecotamide was isolated in toluene.
Yield: 98%.
Example 2:
The isonicotinamide (50gm) was dissolved in methanol (450 ml).Propyl chloride (42 gm) and 10% Palladium on Charcoal (5gm) slurry in Methanol (50ml) was added in autoclave reactor. Autoclave reactor was flushed with nitrogen twice and again flushed with hydrogen. Hydrogen gas was charged 6-8 kg at 40-45°C. Progress of reaction was monitored by thin layer chromatography. Reaction mixture was filtered and washed with methanol (300 ml). Methanol was distilled out and isonipecotamide was isolated in toluene.
Yield: 97.5%.
Example 3:
The isonicotinamide (50gm) was dissolved in methanol (450 ml).Benzyl chloride (46 gm) and 10% Palladium on Charcoal (5gm) slurry m Methanol (50ml) was added m autoclave reactor. Autoclave reactor was flushed with nitrogen twice and again flushed with hydrogen. Hydrogen gas was charged

6-8 kg at 40-45°C. Progress of reaction was monitored by thin layer chromatography. Reaction mixture was filtered and washed with methanol (300 ml). Methanol was distilled out and isonipecotamide was isolated in toluene.
Yield: 97.5%.
Example 4:
The isonicotinamide (50gm) was dissolved in methanol (450 ml). p-Chlorobenzyl chloride (52 gm) and 10% Platinum on Charcoal (5gm) slurry in Methanol (50ml) was added in autoclave reactor. Autoclave reactor was flushed with nitrogen twice and again flushed with hydrogen. Hydrogen gas was charged 6-8 kg at 40-45°C. Progress of reaction was monitored by thin layer chromatography. Reaction mixture was filtered and washed with methanol (300 ml). Methanol was distilled out and isonipecotamide was isolated in toluene.
Yield: 98%.
(The example is for comparison of invented procedure).

Claims
1. A process for preparation of isonipecotamide having formula I

by catalytic hydrogenation of isonicotinamide in presence of platinum group elements on carbon in an organo-chloride solvent, alcohol, non-polar solvent at a temperature in the range of 25-50 °C.
2. A process for preparation of isonipecotamide according to claim 1 wherein platinum group element is palladium or platinum element on carbon or combination.
3. A process for preparation of isonipecotamide according to claim 1 wherein organo-chloride solvent is benzyl chloride, ethyl chloride, propyl chloride or combination thereof.
4. A process for preparation of isonipecotamide according to claim 1 wherein non-polar solvent is toluene, benzene, 1,4 dioxane combination thereof.
5. A process for preparation of isonipecotamide according to claim 1 wherein temperature is in the range of 25-30 °C.
6. A process for preparation of isonipecotamide according to claim 1 wherein the loading of the palladium or platinum element on carbon is 5-10 %.

7. A process for preparation of isonipecotamide according to claim lor 6 wherein palladium or platinum element on carbon is 10 %.
8. A process for preparation of isonipecotamide according to claim 1 wherein in hydrogen pressure is 6-8 Kg.