Why Is the Amine Group in Procaine More Polar in the Para Position?

AI Thread Summary
The discussion centers on the effects of activating and deactivating groups in electrophilic substitution reactions, specifically in the context of procaine, an anesthetic. The confusion arises regarding why the amine group in procaine is positioned para to a deactivating ester group. It is explained that the positioning of substituents affects the polarity of the molecule, with the para position being more polar than ortho or meta positions. The conversation emphasizes that the order of reactions significantly influences the final product. If acylation occurs first, the ester group directs further reactions to the meta position, leading to less desirable products. Conversely, performing nitration and reduction first activates the amine group, favoring the formation of the desired para product during subsequent acylation. The discussion concludes by noting that the energetically favorable product is not always the one formed, highlighting the complexity and strategic nature of chemical synthesis.
nymbler_064
Messages
25
Reaction score
0
I have just been trying to teach myself about the effect of activating and deactivating groups on electrophilic substitution. However, I am a bit confused as to why the amine group in procaine (anesthetic) is in the para position, when the aromatic ring is attached to a deactivating ester. What I am really trying to explain is why the molecule is more polar for having the amine group in the para position, as opposed to the ortho or meta positions.
The structure of procaine is available here:
http://upload.wikimedia.org/wikipedia/commons/thumb/4/4a/Procaine.svg/220px-Procaine.svg.png

Thankyou very much.
 
Chemistry news on Phys.org
Activating and deactivating groups really only affect the reactions that you would perform to synthesize the molecule. In this case, the main product would likely depend on the order that one performs the reactions. The textbook method for generating aromatic amines is a nitration followed by a reduction. To generate esters, it is some kind of Friedel-Crafts acylation.

If one performs the acylation first, the ester group will be meta directing (and deactivating), so the desired product will not be preferred in the nitration.

If one performs the nitration/reduction first, the resulting amine group is both activating and ortho/para directing, so the acylation will be more likely to form the desired product.

Note, however, that these reactions are probably not how the synthesis is performed in practice. I think you would do it like this:

toluene --(nitration)--> p-nitrotoluene --(reduce, reduce)--> p-aminobenzoic acid --(SOCl2)--> acid chloride --(substitute)--> Procaine

The product which is energetically favourable overall is not always the product formed in reactions. That's the beauty of chemistry - it's all about tricking the molecules to do what you want.
 
It seems like a simple enough question: what is the solubility of epsom salt in water at 20°C? A graph or table showing how it varies with temperature would be a bonus. But upon searching the internet I have been unable to determine this with confidence. Wikipedia gives the value of 113g/100ml. But other sources disagree and I can't find a definitive source for the information. I even asked chatgpt but it couldn't be sure either. I thought, naively, that this would be easy to look up without...
I was introduced to the Octet Rule recently and make me wonder, why does 8 valence electrons or a full p orbital always make an element inert? What is so special with a full p orbital? Like take Calcium for an example, its outer orbital is filled but its only the s orbital thats filled so its still reactive not so much as the Alkaline metals but still pretty reactive. Can someone explain it to me? Thanks!!

Similar threads

Back
Top