HOW TO DEVELOP ORGANOMETALLIC CATALYTIC REACTIONS IN API SYNTHESIS: SHORT COURSE

All the information you need to avoid scale-up problems

Date: 16 October - 24 October 2023

Location: Online Platform

Tutors: Dr Vittorio Farina

We are delighted to provide this online course, it will be divided up into four sessions using an online platform. Dates and times are as follows and set in UK, BST (British Summer Time):

Monday, October 16 | 2.00 - 5.00pm BST
Tuesday, October 17| 2.00 - 5.00pm BST
Monday, October 23 | 2.00 - 5.00pm BST
Tuesday, October 24| 2.00 - 5.00pm BST

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, carbonylations and the like. The literature is full of accounts showing that these reactions are difficult to scale up, and sometimes fail in the plant; therefore, it is likely you have experienced these problems. What makes these reactions so difficult to scale up is the fact 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.

With some understanding of the rate law, you will be able to rationally affect important parameters like resting state of the catalyst and rate-determining step; you will be able to select the best ligand at the right concentration for a high-turnover process, you will learn to eliminate performance-limiting off-cycle species, and select the best auxiliary reagent at the appropriate concentration. Many examples will be provided, showing how a certain level of kinetic analysis contributed to a successful scale up, or how such analysis would have helped develop a better process. Specific approaches used to obtain kinetic information will be discussed, including a powerful tool called Reaction Progress Kinetic Analysis (RPKA). All these analyses require surprisingly little effort and theoretical sophistication.

The course will demonstrate that some basic level of kinetic analysis can help optimize the reactions and make them more robust, helping you transfer efficient processes to the plant with increased confidence.

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Speaker: Dr Vittorio Farina