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Benzocaine Synthesis
Benzocaine Synthesis
Benzocaine Synthesis
Aim
This brief write up attempts to illustrate the facile and relatively quick synthesis of
a known local anesthetic, Benzocaine. The target compound will be synthesis
using commonly available materials or which can be acquired with ease.
General info
The reaction
-DCM (optional)
Cleaning
The pills I bought where 500 mg gel caps one, but contained some crap :(
The ingredients where: PABA, Magnesium stearate and rice flour. After a little
reading and thinking I attempted different things in order to get the job done. I
dissolve approx 2g of PABA (and crap) in 90% IPA, shook around, filtered any
solids and left to crystallize. Needless to say I was not impressed, I got some bright
yellow crystals which smelled like perfume, my IPA was full of shit. As I couldn’t
get my hands on some clean one at the moment I read some more and did the
following, which in my opinion is the best I have got so far:
Now all the above can be omitted and I omitted it the first time I did this and I still
manage to get pure Benzocaine, but doing the cleaning now will cut down
other cleaning you have to do latter!
PABA---> Benzocaine
Note: This was my first run and I did not clean the Benzocaine as I
described above, I will be posting the follow up when I have time to see
how the reaction differs with “clean” PABA.
Most of the stuff I have read use a single neck flask, but I like to have
control over what is going on inside so I decided to use a Three neck one.
A Liebig column was use to reflux.
Here we go:
In a 250 ml Three neck flask where placed 1 g of PABA and 7.6 ml of EtOH.
It was lightly heated and swirled so all the PABA dissolves.
When all was dissolved 0.76 ml of 95%
H2S04 where added inside and a white
precipitate formed, stirring was
continued.
I chose the latter one but other people have successfully done the first one.
Tadaaa! 80 mg of un-pure
Benzocaine
As we can see it is red and it is suppose to be white. I tested the red one on my
tongue and it went numb, so yes works but not pure so the following was done:
2) Washed with 100 ml of warm water * a single cold water wash is fine too
3) Dried