PEPAP

[Blammo]

I am posting a potential, easy route to a relatively potent opioid, but I don't know if it is recreational or not.

1-(2-phenethyl)-4-phenyl-4-acetoxypiperidine synth

1-(2-phenethyl)-4-phenyl-4-acetoxypiperidine synth

www.thevespiary.org

First step uses pretty easy to get reagents, alpha methyl styrene, phenethylamine, formaldehyde, and HCl.

Second step acylates the formed product with acetic anhydride, forming PEPAP.

Seems a very simple, straight forward procedure. However I have two questions.

One, how easy would a swap of acetyl chloride for acetic anhydride, or another acyl chloride to replace an ahydride?

I ask because because the potential danger here is that the anhydride dehydrates some of the substrate, which could produce a toxic substrate, a tetrahydropyridine derivative. However, it is also claimed, simply by the wikipedia page on PEPAP, that such byproducts might not be toxic. So idk, as the infamous relative of the toxic by product, MPTP, is utterly terrifying.

I would hope the acyl chloride can be used, and the whole issue averted.

Can anyone speak to such a route?

 

[OneTensionSkyRed]

AcCl is even better for acylation than Ac2O. In the link that you've given someone even writes that they have used propionylchloride for acylation. I have read some literature about MPTP and it's analogues and I think in this case the compound won't be toxic. In order to have toxicity similar to mptp it needs to be N-methylated.