This is from Patent GB 1596874 (http://l2.espacenet.com/espacenet/viewer?PN=GB1596874&CY=gb&LG=en&DB=EPD)
(http://l2.espacenet.com/espacenet/viewer?PN=GB1596874&CY=gb&LG=en&DB=EPD)
Example 2:
6kg of 4-p-chlorophenyl-4-hydroxypiperidine HCl, 2 Kg of KI and 25 Liters of water placed in a 40 gallon ss reactor and covered with Nitrogen. The reaction mixture was stirred, warmed slightly and 3.50 Kg of KOH was added. The mixture was stirred for 5 minutes, 5.95 Kg of y-chloro-4-fluorobutyrophenone enol ether was added and the mixture refluxed gently for from 3 to 5 hours. The mixture was then cooled and 63 Liters of Toluene added , the mixture was stirred for 5 minutes and then separated. 6.4 Liters of Meyhanol was added to the Toluene layer and the mixture transferred to a glass-lined vessel. 2.5 Liters of concetrated HCl acid was added while stirring vigorously, and a flocculent precipitate of Haloperidol(Haldol) HCl separated out. The mixture was stirred vigorously for 5 minutes, cooled and filtered. The residue was slurried with a mixture of acetotone: toluene: methanol and the slurry sucked dry. The residue was again washed with and acetone: toluene: methanol mixture. The residue was washed twice with an acetone: toluene: methanol and the residue sucked dry. The solid was placed in a ss vessel and dissolved in 80 Liters of Methanol , heated to reflux and filtered to a pad of "Hyflo" into a glass lined vessel. 160 Liters of water containing 800 ml of concetrated HCl was added and heated to reflux for from 15 to 20 minutes. The mixture was cooled and 15 Liters of 0.88 ammonia solution was added. The slurry was refluxed with stirring for 1.5 hours, cooled filtered, the residue washed with 2*30 liters of water: methanol mixture, and the residue dried at from 60 to 75°C to constant weight. Yield 7.1 Hg (78% ot the theoretical yield.)
Ok Let's discuss about this.
The Prep of y-chloro-4-fluorobutyrophenone enol ether is also described in GB1596874 (http://l2.espacenet.com/espacenet/viewer?PN=GB1596874&CY=gb&LG=en&DB=EPD)
(http://l2.espacenet.com/espacenet/viewer?PN=GB1596874&CY=gb&LG=en&DB=EPD)
I'm still searching for the synth of 4-p-chlorophenyl-4-hydroxypiperidine. Some additional info is welcome to
You've gotta love me.
My dear Russian and European friend.
The synthesis of quetiapine (seroquel) is described in Patent WO0155125 (http://l2.espacenet.com/espacenet/bnsviewer?CY=gb&LG=en&DB=EPD&PN=WO0155125&ID=WO+++0155125A1+I+)
(http://l2.espacenet.com/espacenet/bnsviewer?CY=gb&LG=en&DB=EPD&PN=WO0155125&ID=WO+++0155125A1+I+)
It0s only alot of printing. (26 pages afortuanatly. Cartrigdes are fucking expensives.)
You've gotta love me.
(xcuse my clumsy English, i'm drunk)
Chromic: only a truly exceptional person, one in a ten thousand, is capable of bluntly stating that he was wrong. Really. This quality is so rare and so indicative of a really remarkable intelligence that every time i encounter it, it makes me feel shy and wanting to apologize :) - please, excuse me if i was a bit over-sarcastic in my post, which i often have a tendency to do :-[ .
Flipper: WOW! Awesome!
Advanced chemistry, no doubt, but i was prepared for that - fortunately, my home city does have a organic chemistry research institute of its own, pretty distinguished in the country, BTW. I mean, i feel quite 'serious' about this project; it's gonna take some time, of course. But then again, it's gonna give some money in return, eventually. Quite a bit of them money, probably.
The only real problem would bee to overcome all the legal restrictions that are imposed on scheduled drugs in Russia.
Anansi: thanks a lot!
I never knew that. Can you, please, elaborate?
I mean - the source of your data (in a PM, if you feel more comfortable this way) and such.
Sufferers of bi-polar affective disorder (sometimes called manic-depressive) seem to be more at risk than people who take it for other conditions such as schizophrenia or schizoaffective disorder.
Actually, although neuroleptics ARE sometimes used in treatment of diseases other than those of psychotic nature, this somehow always seemed to me ............. a bullshit.
I mean, psychiatrists, despite the veil of almost superficial awe that surrounds the medical profession and the hard intellectual labour that is required to beecome a doctor, are so FUCKEN often irresponsible, comletely non-caring people. In addition to that, they - believe me - often prescribe medicines judjing not by their clinical specifications, but by their own intuitive knowledge of 'what kind of high' this or that drug will produce, like "oh, he's agitated and Rohypnol doesn't help, .... well, let's put him on Aminazine, that'll surely fuck him up enough to keep him quiet". You know, this kind of logic - fucking MORONS, so many of them! Not all of them, mind you - just an appreciable amount.
I mean, MDD is just something that SHOULDN't bee treated with neuroleptics. IMHO.
However, the fact that the non-psychotic patients are more susceptible to the dopaminic side-efffects of neuroleptics is immensely interesting, of course, if it's scientifically valid.
Yours,
Antoncho