Pharmacology Nitazenes - The odd N-substitution of...

[4DQSAR]

I'm just wondering aloud if anyone ever tried the (S,S) 2,4-dimethyl azetidine homologue of etonitazene. I mention this because when the diethyl moirty of LSD was replaced by this chiral derivative, the result was more potent than the patent. I've also noted monosubstituted example and so it's possible that like (the S) sec-butyl homologue of LSD, it IS purely space filling as the basic nature of a secondary amine is significantly different to the basic nature of a tertiary amine.

I mean, the former is not going to be economic (so mentioning it isn't going to cause harm) but the latter might suggest that other (chiral) monosubstitutions would be even more potent although, of course, you need that chiral amine so again, it's an extra cost...