Friday, April 23, 2010


the dioxane analog of methylphenidate has never been synthesized to my knowledge, im amazed a pharmaceutical can be allowed onto the market without a more extensive survey of its analogs - what if ethylphenidate is more efficacious? what about propylphenidate? why is it methylphenidate instead of methoxyphenidate? the oxygens would be constrained in the dioxane analog, but i dont know how much movement there is in the first place. what about the phenethylamine analog of phencyclidine? how does DAT inhibition change with tertiary and secondary amines? what about the benzocyclobutyl analog of mescaline, what about dicyclopropyltryptamine, what about DOB-DFLY with one of the oxygens replaced with a nitrogen making it half benzofuran half indole - indole fly?


Pleyadean_Chemist said...

ive been experimenting sythesisizing with methylphenitate i came with some amazing results, took some time and learned a lot, ethylphnidate was the entry point my experiments with MPH.

Dope Amine said...

Funny that you have a picture of 3,4-dichloroethylphenidate! :-) I had been thinking for a while that this material would likely be a good RC candidate.

Considering that ethylphenidate was determined to be a much more enjoyable experience than the dull feeling of methylphenidate, I hoped that the ethyl ester analog of 3,4-dichloromethylphenidate would similarly improve it's effects profile. My primate studies had repeatedly found 3,4-dichloromethylphenidate to be a stressful experience (as well as being significantly more potent than ethylphenidate).

Unfortunately, with the materials readily available the closest analog which could be prepared was 4-chloroethylphenidate (via p-chlorination of ethylphenidate with KCl/Oxone/AcCN). The 3-chlorinated material would have actually been preferred as it should have the closest activity to 3,4-dichloroEPhen but achieving selective meta-halogenation is significantly more difficult. The p-chlorinated product was recrystallized from EtOH, yielding yellow crystalline needles.

Bioassay: Holy shit! This stuff burns the primate's nostrils like no other! No effects noted but this was likely due to the primate's inability to retain enough of the material for adequate intranasal absorption.

Considering this unpleasant aspect, in addition to the more significant fear of the material having neurotoxicity similar to that of 4-chloroamphetamine, it was determined that further planned bioassay experiments should be cancelled.

On to the next experiment....