How to Develop Organometallic Catalytic Reactions in API Synthesis: Short Course

All the information you need to avoid scale-up problems

Date: 01 November - 03 November 2022

Location: Online Platform

Tutors: Dr Vittorio Farina


We are delighted to provide this NEW COURSE online.  It will be divided up into three sessions using an online platform.  Dates and times are as follows and set in UK, GMT (Greenwich Mean Time):

Tuesday, November 1 | 2.00 – 5.00pm GMT
Wednesday, November 2
 | 2.00pm – 5.00pm GMT
Thursday, November 3 | 2.00pm – 5.00pm GMT

If you have helped develop processes to prepare an API, you have certainly come across catalytic reactions such as C-C or C-N cross couplings, homogeneous catalytic hydrogenations, olefin metathesis reactions, hydroformylations, carbonylations and the like. Have you seen cases in which a reaction was run a dozen time successfully in the lab but failed in the plant? If so, you are not alone. What makes these reactions so difficult to scale-up is that the catalysts are unstable and their presence cannot be monitored by the traditional methods, at least if the catalyst is used in very small amounts, which is always the case in a practical catalytic reaction. Therefore, one must resort to some level of kinetic analysis.

The course will go through the most basic situations in which simple kinetic analysis can identify the rate-determining step, the resting state of the catalyst, possible promoters or inhibitors of the reaction (including adventitious impurities like oxygen and water), and whether the catalyst decomposes appreciably. This is all information you will need in order to scale the reaction with confidence.

In addition to the importance of robustness studies, kinetic/mechanistic analysis will help you optimize reactions when the results are not acceptable to you. Do you wish to reduce a side-product formation? Do you wish to prevent a decomposition reaction? Improve catalyst stability? Operate at lower temperature? Kinetic studies will help you address all these situations.

 

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Course Outline

  • The importance of catalysis in the pharmaceutical industry
  • Brief introduction to the field of catalysis
  • Basic concepts: turnover frequency, turnover number, catalyst resting state, rate-determining step
  • Why are catalytic reactions so difficult to scale-up?
  • Why do we need (some) kinetic information?
  • Simple kinetic laws and how to obtain them
  • Traditional methods vs. accelerated methods (RPKA)
  • Pre-equilibrium and steady-state approximations. Saturation
  • Use of precatalysts: why and when?
  • Catalyst inhibitors and catalyst decomposition processes
  • Ligand inhibition
  • The myth of catalyst recycling
  • Homogeneous vs. heterogeneous mechanisms: pitfalls of the black-box approach
  • How to approach the reaction: literature analysis
  • How to run the reaction: catalyst screening for TOF, TON, selectivity
  • How to optimize the reaction: mechanistic information vs. Design of Experiment
  • How to develop the reaction: robustness studies
  • Removing metal impurities
  • The future is here: sustainable catalysis concepts
  • Case studies: application of the principles discussed in this course

Benefits of Attending

You will acquire useful information to develop a catalytic reaction without delving into complex physical chemistry. You will develop tools to optimize and make your reactions robust, so that you will be successful in transferring them to the pilot plant and beyond.

Who Should Attend

Anyone interested in developing practical catalytic reactions using organometallic chemistry. Ideal for less experienced process chemists, but also for those with many years of experience who would like to learn to scale up catalytic reactions with more confidence. It can be useful also to medicinal chemists who need to carry out their catalytic reactions on larger scale.

What's Included

he course fee includes:

  • Link to watch all three live sessions
  • Electronic version of the course manual*
  • Course certificate

For this on line course, there will be no recordings available and *the e reader manual is NOT printable or downloadable (due to copyright).  If you prefer a hard copy of the manual you will have the opportunity of purchasing a professionally printed hard copy during the booking process.

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How to Develop Organometallic Catalytic Reactions in API Synthesis: Short Course

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