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Isophenidine for the Masses.

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Bluelighter
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Apr 12, 2013
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WO 2007/119247 offers a truly wonderful synthesis that runs at RT using non-toxic solvents and very safe precursors.

A closer look reveals that a phenyl-benzyl ketone is reacted with methylamine hydrochloride which is freebased in situ at RT. The hydroxide also removes all of the water produced by the imine formation driving it to the right. So replace each mole of methylamine hydrochloride with isopropylamine hydrochloride. Plain NaBH4 reduces imine to amine.

Believe me, I really did read through some 150 patents to find this because I knew that whoever was making sertraline from sertralone would not want to use TiCl4, nasty, solvents or smelly precursors.

I am sure others will have a better idea than me. It's attractive because it runs at RT, uses methanol as solvent, KOH not only to freebase amine but also to remove H2O.... for someone working in their own space, ideal.

Without a doubt, isophenidine is the best of the series and while the hydrochloride IS soluble, the sulfate is much, much more soluble. I've snorted the hydrochloride, sulfate and phosphate and all 3 were OK as far as we could tell, we had to agree that it IS a LOT like MXE.... apart from the fact that it can be made from cheap, common precursors.
 

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Bluelighter
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I just don't want people to bitch that snorting the HCl hurts - well make the sulfate then! For us, the hydrochloride was fine. I put a 125mg line on my wife's breast and snorted it. Then she put 125mg on my man-boob and snorted it....
 

dopamimetic

Moderator: N&PD
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Do you refer to this:
1. WO2007119247 - IMPROVED MANUFACTURING PROCEDURE FOR THE PREPARATION OF POLYMORPHIC FORM II OF CIS-(1S)-N-METHYL-4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-1-NAPTHLENEAMINE HYDROCHLORIDE (SERTRALINE HYDROCHLORIDE)
?

As they are cracking down on RCs throughout Europe now, guess I finally need to indulge in learning more solid chemistry. No way that I'll stick to expensive toxic, illicit K or do these once-a-week administrations in a clinical setting.
 

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Bluelighter
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Do you refer to this: ?

As they are cracking down on RCs throughout Europe now, guess I finally need to indulge in learning more solid chemistry. No way that I'll stick to expensive toxic, illicit K or do these once-a-week administrations in a clinical setting.
The paper & books is 1200+ pages and that still covers less than 50% of scaffolds for strong opioids. Even the Eunoia disc is out of date. The few hundred thousands patents were made before QSAR was understood so 4-phenyl propiram (for example) overlays fentanyl perfectly but it's LogP isn't quite as good so only x60 morphine.

I guess I am simply angry to see bad crap sold because it's the cheapest and easiest to make... That's why I put the isophenidine 1-pot synthesis out there. There are a STACK of possible precursors and preprecursors (the later technically legal and I LIKE legal).
 
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