Dexethylphenidate, Dexisopropylphenidate & Pexpropylphenidate

[Nexus_Tripper]

Is it possible to make dexatory analogs of RC phenidates? And if you can make them, why is are all of them that are available the shit racemate? It seems like drug makers are idiots that don't care about quality... I betcha that the LSZ that was recently sold wasn't the true SS enitomer. I've made LSZ and 75mcg the pure SS isomer felt like 100-125mcg of LSD. And it had far less body-load, unlike the shit public LSZ.

 

[neurotic]

it'd be easy if one started with dex-methylphenidate from Focalin, but RC chemists probably don't go by that route? idk

 

[sekio]

nobody wants to add a chiral resolution stage in a drug where the enantiomer has been proven to be functionally inactive & rapidly metabolized

 

[serotonin2A]

it'd be easy if one started with dex-methylphenidate from Focalin, but RC chemists probably don't go by that route? idk

They are definitely not starting with d-methylphenidate, which is considerably more valuable then ethylphenidate, and controlled.

To the OP, there is no economic incentive for RC companies to sell the d-isomers. In addition to the added expense of chiral seperation, they would loose at least half their product.

Drug companies didn't even start producing d-methylphenidate until recently, even though methylphenidate has been on the market for years. Does it really suprise you that RC companies would act any differently?

 

[sekio]

It seems likely that the commercial -phenidates are (+/-)-threo compounds. A synthesis producing exclusively threo- isomers is easy enough.

Levomethylphenidate is actually rapidly destroyed by esterase enzymes and is ten times less potent as a stimulant than dexmethylphenidate; when orally administered it doesn't actually make it to the brain, and if it did it wouldn't be effective. Even when administered in ways that bypass first pass metabolism, the rapid destruction of l-methylphenidate means it will have a short half life and minimal overall activity. (ref) I suspect the same holds true for the other -phenidate esters.

Curiously enough, the high affinity of L-methylphenidate for esterases means that L-ethylphenidate (and not D-ethylphenidate) is the major product that forms transiently in the body when it's coadministered with ethanol. Although that, too, is destroyed rapidly.