Manufacturing process for methyl phenidate and intermediates thereof
AssigneeIPCA Laboratories Ltd.
InventorsAshok Kumar, Dharmendra Singh, Swapnali Hemant Patil, Ganesh Devidas Mahale, Uttamrao Arjunrao Sawant
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Abstract
The present invention discloses selective and complete reduction of pyridine ring in a biaryl system comprising ∝-substituted or non-substituted benzene ring and relates more specifically, not exclusively, for the manufacture of methylphenidate, which is used for treatment of Attention Deficit Hyperactive Disorder (ADHD) and also acts as central nervous system stimulant, by using palladium/C in a solvent such as C1-C4 alcohols in presence of molar quantities of organic and/or inorganic acids.
Claims16
A process for reduction of a compound corresponding to the general Formula I, wherein R denotes CONR1R2, COOCH3, or COOH;
- X denotes hydrogen, Cl, Br, Ome, or NH2;
- R1 & R2 are independently Hydrogen or C1-C3 alkyl groups,
- said method comprises the steps of:
- a) preparing a reaction mixture by mixing
- i) a compound of Formula I, wherein R, X, R1 & R2 are as defined above,
- ii) an organic or inorganic acid,
- iii) one or more alcoholic solvent, and
- iv) palladium catalyst:
- and
- b) effectuating reduction of said reaction mixture in a hydrogen atmosphere to produce a reaction mass comprising compound of Formula II.
The process as claimed in claim I, wherein the reaction is carried out at a temperature of 35° C. to 70° C. and a hydrogenation pressure of 5 kg/cm2 to 15 kg/cm2.
A process for preparation of methylphenidate or a derivative or a salt thereof comprising a step of reducing a compound of Formula I in presence of a palladium catalyst
- wherein R denotes CONR1R2, COOCH3, or COOH;
- X denotes hydrogen, Cl, Br, OMe, or NH2;
- R1 & R2 are independently Hydrogen or C1-C3 alkyl groups.
Dependencies are inferred from the claim text.