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 Peter Takes on History 

March 9, 1899

Felix Hoffmann's Penchant for Acetylation

Today, March 9th, is the feast day for Saint Frances of Rome – the patron saint of Automobile drivers. As any Catholics here can affirm, there are saints for any occasion. St Adjutor is the patron saint of swimmers. St Bernardino of Siena is the patron saint of advertising. Here’s one I remember from high school; St Drogo the patron saint of unattractive people. Here’s one I hope none of you know. St. Julian the Hospitaller. He dedicated his life to providing hospitality for the sick and needy. Nice guy right? Well, actually it was kind of make-good after he killed his parents. St Julian the Hospitaller is the patron saint of murderers.
Greek gods are the same way; one for every occasion. Aristaeus - the God of bee-keeping, Epimetheus – the God of excuses. And Poine - is the goddess of revenge and punisher of murderers! So, maybe the Goddess Poine is the one who got ahold of St Julian, right?
The Goddess Poine - thru a few millennia of etymological shapeshifting - Greek to Latin to Old French and Middle English - she gave us the modern word for pain and pain shares the same root as the word penalty; a connection that illustrates an ancient connection. Pain was often considered punishment for human sins or human folly. It wasn’t until the Renaissance that Rene Descarte proposed pain as a signal of a malfunction in the human machine.
But whether from within or without, people in pain have been willing to do almost anything to get out of it. You gotta figure the guy was in a lot of pain who said, “OK, yes, acupuncture sounds reasonable.” Yet 3000 years later, millions still say yes.
Actually, surprisingly, many ancient methods of pain relief have a grounding in science.
In 2500 BC ancient Egyptians used electric eels for healing. We’ve learned the effect isn’t much different from modern Transcutaneous Electrical Nerve Stimulation.
We can also thank the Egyptians for leeching. Turns out, not all as crazy as it sounds. Analysis has shown that the leech’s saliva contains anesthetic that can numb wounds and contains a very raw form of an anti-inflammatory drug that’ll hang around in the Leech-ee’s system.
4000 years ago weekend warriors in the fertile crescent began chewing Willow Bark for pain relief and, as most of you know, they were on to something. Some plants of the genus Spirea contain Salicin, the main component of salicylic acid, an effective analgesic.
So for, literally, thousands of years people knew of the pain relief found in chewing willow bark but, chewing willow bark has some drawbacks. It can upset the tummy, there’s the nausea and possible kidney inflammation and, well, you’re chewing on bark.
So chemists started trying to isolate the active ingredient but it wasn’t until 1887 when a young chemist named Felix Hoffmann managed to formulate a clean and stable form of salicylic acid by acetylating the compound. And on this day in 1899 Hoffman, an employee of Germany’s Bayer Chemical, patented Acetylsalicylic Acid that would be marketed as Aspirin. "A" for "acetyl" and "spirin" for Spirea.
Now, Bayer knew that they had a hit and immediately tried to patent it. The German government refused because other folks in the past had formulated Salicylic Acid. The US patent office recognized that the real trick here was Hoffman’s acetylation and granted a patent for control of the drug in America turning Bayer into one of the richest corporations in the world.
Now, I mentioned acetylation a couple of times. I read up on it to see if I could explain what it is. Turns out, no. Something about making compounds less disruptive to body chemistry and more effective in the manufacture of proteins. Yadda, yadda. But I can tell you this, Felix Hoffman was acetylating everything he could find and had another hit. Folks just can’t get enough of his acetylated morphine. We call it heroin.

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