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Innovation & Technologie Angebot

Innovative continuous-flow process for the preparation of methylphenidate hydrochloride

Country of Origin: Belgium
Reference Number: TOBE20170627001
Publication Date: 27 June 2017

Summary

A Belgian research university has developed an innovative  continuous-flow process for the preparation of methylphenidate hydrochloride. This molecule is the active ingredient of medication  prescribed worlwide to treat attention deficit hyperactivity disorder (ADHD) and narcolepsy. The process is safer, cleaner and faster.  A licence agreement or a research agreement are sought.

Description

Methylphenidate hydrochloride, a central nervous system stimulant, is the active ingredient of medications such as Concerta, Ritalin, Metadate, Methylin,… that are amongst the most widely prescribed stimulant medications to treat attention deficit hyperactivity disorder (ADHD) and narcolepsy (2,4 billion doses per year in 2013).
The methods used for the preparation of this molecule are mainly based on stepwise macroscopic batch processes which come with various shortcomings (poor mixing…) ultimately accounting for low productivity, quality deficiency and poor flexibility.
Besides, an increasing chemical risk is associated with classical large scale, stepwise batch processes, in particular when highly reactive species or hazardous/explosive intermediates are involved.

The Belgian research team patented the technology which relates to a scalable, safe and intensified continuous-flow process in micro/mesofluidic reactors for the production of methylphenidate hydrochloride. Besides, the patented invention provides various methods for synthesizing some specific pharmaceutically active species (reaction intermediates of methylphenidate synthesis), by using continuous-flow conditions with a drastically improved efficiency by comparison to the batch procedures.
The research team is looking for licence agreement and/or collaboration research agreement for development/optimization of continuous-flow production process(es) of other compound(s).

Advantages and Innovations

The technology consists in an alternate more cost effective process to produce methylphenidate hydrochloride, or to synthetize any of its reaction intermediate:
.- overcomes the shortcomings of the batch processes : better mixing and heat transfer,
- accurate control on the reaction conditions, improved yield production and obtention of a product with a constant quality and purity profile
- safer process
- faster process (few minutes instead of few hours)
- cleaner process (minimal footprint)

Stage Of Development

Under development/lab tested

Stage Of Development Comment

Continuous-flow conditions of the whole methylphenidate hydrochloride synthesis process were optimized at microfluidic scale in lab (production yield around 20 g / day scale). 

One critical reaction step of the process was validated on a commercially available pilot mesoscale continuous-flow reactor enabling a productivity of 4.25 kg / day.

Requested partner

Licensee partner who would like to produce methylphenidate hydrochloride by using the patented optimized continuous flow process.
Collaboration partner who would like to develop and/or optimized other continuous flow process for the production of other compounds on the basis of the patented production process.

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