Spiridone

[haribo1]

Here is a tasty morsel. 202x morphine with a duration of 48 hours. The synthesis is trivial.

Actually, is it worth listing each opiate class with the strongest known member of that class as example?

 

[Ham-milton]

It'd certainly be interesting.

I wonder why spiridone hasn't been investigated for opioid addiction

 

[haribo1]

I imagine because it's still cheaper to make methadone. I said the synthesis was trivial; it is, but not cheap.

 

[dorothyperkins]

It must be so much more potent than methadone though. What does 202x morphine translate to for methadone? The duration must be longer too, i know methadone has a long half life but probably not that long.

So assuming its 200x the potency of methadone and lasts twice as long, it would have to cost 400x more per gram before it became less profitable? You have to invest money initially to convert your plant to be able to produce it but the potential profit must be pretty huge.

 

[Ham-milton]

I think that your 200x potency of methadone is pretty accurate for chronic dosing, anyway.

I wonder if this would build up in the liver the same way methadone does.

 

[Ham-milton]

I'm looking at this compound today after just randomly drawing chems that could match the morphine rule and drawing the 'spiro' end of it.

I realized that spirodone actually matches the morphine rule going in both directions from the amine. Obviously the usually diphenylheptan-3-one's are pretty well researched, but what about simpler spiro-type chems matching the morphine rule (ie: going in the spiro direction).

another, entirely unrelated question, is this actually 'make-able'?
tetraspiro[5.1.58.1.515.1.522.16]dodecasiloxane

 

[immaturepoop]

Actually, is it worth listing each opiate class with the strongest known member of that class as example?

That'd be interesting AND informative - from a pharmacologic standpoint. An area I could use more help in, hahaha. Synthesis is what really tickles me, and Spiridone's structure is quite interesting considering the potency. and I'm curious as to how 202x morphine translates to methadone also... hmmm

 

[MurphyClox]

Here is a tasty morsel. 202x morphine with a duration of 48 hours. The synthesis is trivial.

Where did you get these values from? I hardly find anything about that one in SciFinder...

Edit: J Med Chem 1978, 21, p.474 maybe ?!

 

[MurphyClox]

another, entirely unrelated question, is this actually 'make-able'?
tetraspiro[5.1.58.1.515.1.522.16]dodecasiloxane

Not very likely. One major problem would be adjusting the ring sizes. Second is purification (ok, that doesn't exclude "make-able").
Also, you've got free SiH2-groups, which are prone to oxidation at the first sight. Silicium is said to be very "oxophilic", so these groups are thought to be attacked by the next oxygen available and we got some in this molecule...

I admit, I'm far away from being an expert in silicium chemistry

Peace! Murphy