Conversion of Oxycodone to Oxymorphone

by Epikur

It seems a number of bees have access to oxycodone. Once this compound is available, one would immediately dream of converting this compound into the far more potent oxymorphone. This would increase the potency by a factor of 15 when based on intramuscular application.

Most processes to split off the O-methyl in codeines are quite messy, the yield is low, expensive or hard-to-get chemicals are required ... and a lot more worries which makes it usually not parctical to do for bees. But now yours truly has now found a process TO DO IT in a process adaptable to kitchen chemistry. All chemicals are cheap and unsuspicious.

Here is the procedure

A mixture of 3.15 g (10e-2 mole) of oxycodone, 28.3 g (3.1e-1 mole) of methanesulfonic acid and 2.2 g of DL-methionine are heated to 40° C. The reaction mixture is stirred at this temperature for 12 hours and then poured onto ice. The mixture is made alkaline with ammonia to a pH = 8 to 9, then extracted with dichloromethane. The organic phases are washed with water, dried over sodium sulfate and evaporated to dryness under reduced pressure. The crude product thus obtained (2.51 g) is purified on a column of silica by eluating with pure chloroform followed by a gradient with methanol. 2.17 g of oxymorphone are thus obtained, which represents a yield of 72%.

You will most likely want to convert this into the hydrochloride: 5 g of the purified base previously obtained are disolved in 30 ml of warm acetone. After concentration to about 10 ml, 5 ml of 6N hydrochloric acid are added to the warm solution. The mixture is cooled to -10° C, and the precipitate is filtered off, washed with acetone and dried at 50° C in a vacuum. 4.83 g of oxymorphone hydrochloride are thus obtained. Yield 87%.

With an overall yield of 63% and a potency increase of 15, the actual gain factor is around 9, i.e. you have 9 times more opioid activity than at the beginning. A one-day dose can therefore be converted into a week-dose. No bad, eh?

The kitchen chemistry adaptions would include the use of a hair dryer insted of the reduced pressure, skipping the purification process (the crude product should be clean enough and no toxic chemicals have been used).

I already know your next question: will it work with codeine or other codeine derivatives like dihydrocodeine or hydrocodone? NO, it won't. The yield would be terribly low (~15%) and a lot of goo is formed so serious cleanup has to be done.