31 October 2009

Whose Profits Would Home Made Sublimaze Threaten?

What is the point of importing heroin when sublimaze (fentanyl) will suffice?

This just doesn't make sense; is heroin so cheap that it is cheaper to import rather than manufacture a more potent substitute, ie fentanyl?

Instead of seeing headlines such as, "Homegrown Pot Threatens Mexican Cartels; why aren't we seeing, "Heroin Substitute Fentanyl Threatens Afghan Heroin Industry"?

Fentanyl (sublimaze) is also relatively easy to make. Assuming you have a lab and can get hold of the chemicals, it would be economically viable to make this compound in a back street lab: unlike for example, amphetamines.

There are a number of synthetic routes on the internet. For example, the DEA write about the original Janssen route (Janssen were the company that invented the compound) and a route based upon N-phenethyl-4-piperidone. Whilst other sources also suggest the N-phenethyl-4-piperidone route.

If I were to make this compound I'd also go with this route, except, it presents a tiny problem. How do you make N-phenethyl-4-piperidone?

Our internet chemists suggest, for example, that "N-Phenethyl-Piperidone (NPP) which can be easily synthesized from Piperidone and Phenethyl-Tosylate or Phenethyl-Bromide."

Well, in principle, yes. But here's how I would make it.




Take some phenethylamine (either bought or made from LiAlH4 reduction of benzyl nitrile) and react with slightly over two equivs of ethyl acrylate to give the Michael product which can undergo condensation in the presence of alkoxide base. Acidification and decarboxylation takes us to N-phenethyl-4-piperidone.

This strategy can be seen on page 147 of Warren.

Once this compound is in hand, I would follow the given route (most probably telescoped) of aniline imine formation, and subsequent sodium borohydride reduction, followed by propionate amide formation.

Perhaps the paper titled, "A Convenient One-Pot Synthesis of Fentanyl" (DOI: 10.1002/chin.200549130), is the route above? I don't know. The authors haven't published in an open source journal which suggests that they don't want to be read; I'm avoiding taking up an Athens account in order to maintain some sort of solidarity with the disenfranchised. If anyone knows, please drop me a line.

1 comment:

  1. amazing info- would love to read something broken down into laymans terms

    ReplyDelete