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Make piperonal from piperinic acid - Video Tutorial

Make piperonal from piperinic acid

We know you've been waiting for this one.

We've been playing around a bit and we're now going to show you the next step in our

reaction sequence that started all the way back with white peppercorns.

Just to recap, first of all we extracted piperine from white pepper using ethanol, and recrystallised

it.

We then took the piperine and hydrolyzed this in an ethanolic alkali solution to form piperidine,

which we separated, and piperinic acid.

So here's a couple of samples of piperinic acid that we've obtained.

The one on the left is very clean and yellow coloured, and originates from white pepper.

The one on the left is slightly more brown coloured and originates from black pepper.

There's obviously still a little bit of the dark colouring that's made it all the way

through the process.

We're going to use the darker sample for this experiment, but there's really no difference.

So here goes, our starting material which is 3.7 grams of piperinic acid, prepared as

per our previous experiment.

It's lumpy looking, but it's quite a dry solid as you can see.

Here's the chemical structure.

What we're going to attempt to do is a fairly violent oxidation reaction where we'll try

to oxidise the two double bonds in the side chain of the molecule, and the result will

be various different products, however we're hoping that one of them will be piperonal,

an aromatic aldehyde.

1.

The first step is to get the piperinic acid into aqueous solution.

To do this we're going to convert it into the sodium salt which is water soluble.

So here's 0.69 grams of sodium hydroxide.

The same molar amount as our piperinic acid.

We'll make these into a solution using a large beaker which will end up being our reaction

vessel.

We'll need at least 700 mils of volume in here.

And we'll use 100 mils of water to get these into the solution.

Use a large stirrer as stirring is important for the reaction.

First we'll add the piperinic acid.

As you can see, it's pretty much insoluble in water as it is in the acid form.

So now we'll add the sodium hydroxide to the mixture.

Immediately you can see the color change and the solids start to dissolve.

Normally the solution is a yellow color, but we've obviously got dark colored impurities

in here so we've got a darker colored solution.

Get the stirring up, and leave this for 10 minutes to make sure that everything has dissolved.

The mixture goes a little foamy.

If after a few minutes you've still got lots of solids in there, you can add a little bit

of hydrogen peroxide.

Then it's possible your previous hydrolysis step wasn't complete and you've still got

piperine in the mixture.

This is looking good though.

So the next step is to prepare our oxidizing agent.

We've played around with a few things here and we've got a combination which gives a

fairly low but reasonably consistent yield.

So here it is.

Double trouble.

On the left we've weighed out 3.9 grams of potassium periodate.

One mole equivalent.

We prepared this in previous videos, starting all the way back from iodine, so go back and

take a look for more info.

And on the right we've got 5.4 grams of solid potassium permanganate crystals.

This is two mole equivalents compared to the piperinic acid.

Permanganate on its own can apparently be used for this reaction, but we've tried it

and we get lower yields than with this combination.

We think that these reagents work in conjunction to perform the oxidation process and break

those two double bonds up.

In the first step, permanganate reacts with a double bond, forming a diol as an intermediate.

This will then react further with both permanganate and periodate to break and form two carbonyl

compounds.

Neither of these are very soluble in water, and in addition we want to keep the concentration

of the mixture low in order to minimize excessive oxidation.

So we've got a combination of these two.

So here's 500 ml of water at about 20 degrees C. Let's go.

It takes a few minutes before the crunching sounds go away and we've got a deep purple

colored solution.

Ok here we go!

This is now ready to kick some double bond ass.

We've got our two reactant solutions ready.

We need to prepare one more thing though.

One of the risks with this reaction is that the products are themselves very prone

to oxidation.

So we need to stop the reaction after a period of time and quench any excess oxidizing agent.

Ok... we're good.

We'llestrapped.com.

on the left we've got 2.1 grams of solid sodium hydroxide and on the right 5.3

grams of sodium bisulfite which is sodium hydrogen sulfite we'll get these

dissolved in about 75 mils of water

together these will form sodium sulfite in solution which is our reducing agent

to quench the reaction they dissolve easily note that we don't use sodium

bisulfite itself to quench because although it would work it could also

react with our aldehyde product to form an adduct which we don't want okay well

that's a lot of preparation for a reaction but it's worth spending the

time to get everything ready here's our three solutions let's start with our

sodium piperonate solution in the large beaker

you

just to help moderate the reaction a bit we add three ice cubes to this and

start stirring

stir the oxidizing agent solution with a glass rod and make sure that there's no

solid settled on the bottom and now with vigorous stirring we add this to the

piperonate solution

and we're going to wait now for two minutes for the reaction to proceed you

can see a color change starting to take place in the mixture and a brown color

forming there's also a brown colored precipitate once you see this on the

sides of the beaker it's time to stop the party here we go after about two

minutes

so now we add the quench solution

so now we add the quench solution

so now we add the quench solution

pretty soon the mixture starts to settle

pretty soon the mixture starts to settle

and you can see a light colored solution

and you can see a light colored solution with a fairly heavy precipitate in it so

let's start by filtering this and

separating the filtrate from that

separating the filtrate from that

precipitate

We first wash the precipitate with a little

water.

Then once it's relatively dry, we're going to wash it using an organic

solvent to make sure that we've got any possible products out of here. We'll use

two portions of 30 mils of dichloromethane and wash the precipitate

thoroughly with each one.

we now take the filtrate and place it into a separating funnel hopefully it

will just fit. There's a nasty black precipitate left in the filter but we're

not totally sure what it is. It's not manganese dioxide, so it might be organic

by-products or something. There's a nasty black precipitate left in the filter, but we're not totally sure what it is. It's not manganese dioxide, so it might be organic by-products or something.

some other insoluble product the DCM forms a nice obvious bottom layer we

shake the mixture up for a minute to allow maximum extraction and then let it

separate again and we separate the bottom DCM layer

we do another extraction of the aqueous mixture in the funnel using another 15

minutes just to demonstrate the aqueous mixture left in the funnel is still

fairly alkaline what this means is that any acidic byproducts over oxidized

compounds or starting material from the reaction should have remained in the

aqueous layer here's our DCM extract we dry this using a small amount of

anhydrous magnesium sulfate

and then evaporate off the solvent let's see what we get

we get an oily residue which at room temperature solidifies and forms a

beautiful crystalline mass the melting point is somewhere just above room

temperature but we'll come on to this in a moment it's all solid as well with no

oily component remaining so enjoyed the view from the DCM extract video if you liked this video please subscribe to my channel and hit the bell icon to get notified of future videos

a minute or two and then broke up the solid and scraped it out of the

container

it's quite solid and crystalline as you can see not really waxy at all

and this is our crude product 0.5 grams exactly of crude pipe ronal as a yellow

colored solid this is a yield of 20%

from the starting piper inic acid nothing spectacular but it's the best

we've been able to manage from this reaction but it's still worth it why well

the aroma is simply incredible the first thing that hits you is a wave of

jelly belly toasted marshmallow beans it's got that buttery richness to it and

it's slightly vanilla like as well but it's also got a fruity edge to it as

well like maraschino cherries

overall like a rich homemade cherry bakewell tart with almonds vanilla

cherries butter and toasty aromas Wow and what's fascinating is having been

through the process first of all from the spicy white pepper the fruitiness of

the pure pipe rind then to the relatively unscented piper inic acid and

now to this beautiful concoction okay we know what you're thinking cut the poetic

bullshit and show us some proof okay here's our

DIY melting point setup let's get some product in the tube and a thermometer in

there and set up and we'll warm this now very very slowly and gently at 27 degrees

C now and the product in the tube is still completely solid getting up

towards 30 degrees and soon we've got our first sign that something is

happening there's some solid that looks wet on the side of the tube and what's

and we've definitely got the start of a melting point range here temperature is

34 degrees C and now it's completely melted 37 degrees C well the textbook

says 37 degrees C for pipe ronal that's pretty impressive our measurement is

slightly on the low side but it melts pretty sharply and it's very close so

ladies and gentlemen this is the real deal we're really pleased we did get a

way to go all the way from peppercorns to pipe ronal even though the yield is

not great it's something we really hoped we could achieve and capture on film

there are probably other ways to do this but copper sulfate didn't work for us

and plain permanganate was lower yielding and unpredictable

stay tuned