kilomentor

Creating rugged scaleable processes has always been important for process chemistry. Exploratory and early development small scale reactions are most frequently purified using chromatography, but chromatography is not readily scaled up and it is expensive. Larger scale requires more rationally selected purification methods. A goal of this presentation is to show how using sulfuric acid esters can efficiently and economically improve preparative scale organic synthesis.

I have proposed that a synthetic chemist can assess the relative merits of two or more routes of synthesis by looking at the proposed intermediates in the schemes and rating the likelihood that they can be separated cleanly and in good yield. Schemes that have a higher proportion of these preferred intermediates on balance are more promising. One intermediate that I propose that you can depend upon being readily isolated and efficiently purifiable is salts of organic acids and bases. Below I would like to may a variety of points which all apply to using salts of carboxylic acids as dependable intermediates.

The Goal of the Kilomentor Blog is to build up a body of information over time, which can be alternately described as:

• a free school teaching chemical process development
• free chemical process synthesis training
• no cost industrial chemistry education
• complimentary fine chemical or pharmaceutical mentoring
• kilo or engineering scale chemical process instruction
• complimentary chemical synthesis teaching

I am a graduate from Harvard University and have worked for more than 40 years as a pharmaceutical process chemist in Canada and the United States. My motivation is to remove every barrier preventing chemists, anywhere that the world wide web reaches, from improving their process chemistry talents. Just search the keyword kilomentor!

Based on an examination of what really goes on in a chemical process step a method of rating the difficulties of the separation are proposed as a quantitative tool to rank the challenges of a process scale up.

Nature to be commanded must be obeyed.

In synthesis we talk about assembling, building or constructing a molecular structure. In an important aspect this is a misleading metaphor because we are comparing an activity in the nano-world to an activity in the macro world. Operating in the macroscopic world, as for example in building a house, we handle the pieces, we position the pieces, we join the pieces.

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Any process has the possibility of continual incremental improvement but practically a point will be reached when it is not worth further effort and one’s time and talents are better expended elsewhere.

One key to imaginative and rugged chemical process development is extractive separations which are general for functional groups besides acids and bases. Many years ago now, a short paper was published which taught how to selectively extract only aldehydes. into water as areversible complex and thence isolate them.

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• Symmetrical Bis-N,N-(3-nitrophenyl)urea: A Super Co-crystal Former that might have applications in Product Purification.
• The Importance of the Molecular Weight of a Salt Former in choosing a Pharmaceutical Salt
• Reiterating the Objective of the Kilomentor Blog
• The process vision: an integrating strategy in pharmaceutical process development
• Phosphate Pharmaceutical Salts : Chemical Process Development & Organic Synthesis
• Green /Recyclable Solvents: Low Vapour pressure compositions for storage and recycling of solvents that are highly volatile or gaseous at room temperature
• Sulfate Pharmaceutical Salts
• Making the Hydrochloride Pharmaceutical Salt of Basic Drug Substances
• Kilomentor weighs in as “Pharmaceutical Manufacturing Goes Green”.
• Another Way to Separate Phenolics by Crystallizing of Co-crystals?
• The Complete Blog for the Preparation of Pharmaceutical Salts
• Inverted Filtration: A chemical synthesis laboratory technique particularly helpful at 5-10 litre scales.
• Recovering More Product by Crystallization in Organic Synthesis:Trituration with a Modified Water Phase as a Potential Chemical Process Development Method
• Kilomentor moves the discussion from Steam Distillation to other Co-distillations
• Polymorphism in Organic Syntheses, Process Development and Formulation

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