4-F-MCAT

tetraedr · Sun Jun 19, 2005 1:41 am

The other 4-fluoro analogues of amphethamine and methamphethamine were presented here:
https://www.synthetikal.com/synthforum/viewtopic.php?t=756&sid=5df29cd644a38c41221712d54b7a8752

In this topic I want to present the last work in this group - 4-fluoro-methcationone analogue.

4-F-MCAT
To the boiling solution of 5.75 g (37.78 mmol, 1 eq) of 4-fluoropropiophenone (purchased from Acros Oranics) in 20 mL of methanol was added dropwise 6.34 g (39.67 mmol, 1.05 eq) of bromine very slowly. The solution have to be becomes light yellow quickly between bromine drops. After complete addition through this solution was bubbled the air during 1 min (for removing the rest of HBr), then it was cooled down, diluted with 100 mL of cool water and vigorously stirred for 1 min. Then, almost all water was decanted from heavy oily layer of 4-fluoro-alpha-brompropiophenone and 3.83 g (56.67 mmol, 1.5 eq) of methylamine hydrochloride was added followed by 40 mL of benzene. This mixture was warmed to 60-70OC, solution of 4.24 g (75.56 mmol, 2 eq) of KOH in 10 mL of water was added there and resulted mixtures was kept at this temperature for 2-3 h with vigorously stirring. The color becomes lemon-yellow. After cooling the benzene layer was separated, water layer was extracted with 10 mL of benzene, combined organic layers were washed with water and extracted with mixture of 4 mL of HCl and 4 mL of water, then, one more time with 1 mL of HCl and 1 mL of water. Combined water extracts (dark brown-green color) were diluted with IPA, evaporated, then co-evaporated one more time with mixture of IPA-benzene. Obtained crystals was filtered with ether, washed several times with ether until clear white color. Yield – 2.56 g (31%). After evaporation and re-crystallization of mother liquors is possible to get some more of product.

The preliminary data of bioassay will be a little bit later, but they not so interesting. 4-FA and PFMA data seems better.

MargaretThatcher · Sun Jun 19, 2005 5:00 am

Thanks, another excellent one. The cathinone analogues are really interesting. Shame that you say the assay isn't interesting but look forward to the report.

Vitriodor · Sun Jun 19, 2005 7:32 am

Nice write up Tetraedr! Very clear description of what has been done.Were you able to meassure the melting point of this compound?

tetraedr · Sun Jun 19, 2005 8:55 pm

So... I will make m.p. and NMR data of this compound next week, naturally!

And here I present announced the bioassay data (my translation - sorry for my English):

Volunteer – the man about 40 years old. Many years he used the methedrine and other similar stimulators in big amounts.

12:45 – 200 mg of 4-F-MCAT intramuscularly as 2 ml 10% soln.
12:50 – Spontaneously slaver, noise in the ears, euphoria started.
12:51 – Something like incoming, but weak…
12:52 – Increase of the action, brokenly breath.
12:54 – Light euphoria, sweating started.
12:55 – Light psychedelic nausea, Euphoria increased quickly.
12:56 – The eggs draw in.
12:57 – Empathy appeared, metallic taste in the mouth.
12:59 – Blood pressure increased a bit, slaver decreased, noise in the ears disappeared. Sweating stopped, empathy increased a bit, light euphoria. No visuals.
13:00 – Deep breath drive away all effects. Probably, dosage 200 mg was not enough?
13:05 – No changes
13:08 – Intensive increase of stimulator’s effects. Very light euphoria. The face feels like rubber. No problems with typing it on computer.
13:22 – No changes.
13:31 – Decreasing all actions.
13:40 – Light post-action. The condition almost normally.
13:55 – One more 200 mg of 4-F-MCAT.
13:59 – Increasing the action, strongly, than last time. Noise in the ears.
14:00 – Pleasant hot wave on all body.
14:06 – Euphoria increased strongly.
14:14 – The feeling like “not enough dosage”. Sweat again, the voice become hoarse.
14:22 – Not enough euphoria.
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The action finished about after 2 hours. Empathy was low. The estimated normal (full) dosage of 4-F-MCAT is 400-500 mg. 4-FA and PFMA seems better than this cathinone.

tetraedr · Wed Jun 22, 2005 11:30 pm

Some new physical data of this compound: m.p. about 240 grad (with sublimation).

NMR-1H (DMSO-d6) ppm: 1.46 d (3H, Me), 2.58 s (3H, NMe), 5.14-5.20 m (1H, CH), 7.42-7.46 m (2H, Ar-CH), 8.12-8.16 m (2H, Ar-CH), 9.57 bs (2H, NH2+).
Not aryl signals very close to the same signals at ordinary methcathinone.