|
|
| Author |
Message |
Klot
|
| Joined: 14 Feb 2005 |
| Posts: 93 |
|
581.06 Points
|
|
|
Tempidone
Mon Feb 14, 2005 6:35 pm |
 |
|
2,2,6,6-tetramethyl-4-piperidone (Tempidone) may be found OTC from "Templagin"
If you have references for activity fentanyl analog from whis piperodone ?
Sorry for my bad English/ |
|
| Back to top |
|
 |
|
|
|
syn
Wed Feb 16, 2005 10:03 am |
|
|
Do you mean what is the activity of Fentanyl?
Okay,
http://www.ch.ic.ac.uk/ectoc/echet98/pub/028/
http://www.csen.com/anesthesia/lollipop.htm
The rank order of potency of the drugs studiedwere; etorphine > hydromorphone > dezocine > xorpha-nol = nalorphine = butorphanol = lofentanil > metazocine> nalbuphine > cyclazocine > fentanyl > morphine >>>>&--946;-endorphin. As can be seen, the rank order of efficacy wasnot related to the rank order of potency. In fact one of themost potent ligands, xorphanol, was the least efficacious.
Hope this helps
Fentanyl, is relativly safer analogue to make, then say etorphine, or carfentanil,
If for example you made a mistake, in the sysnthesis of carfentanil, breaching only a fraction in would kill you,
Carfentanil is 10000x more potent g/g than Di-acetyl Morphine(heroin), fentanyl is 1000x that of Heroin
syn
Last edited by Guest on Fri Feb 18, 2005 10:09 am; edited 1 time in total |
|
| Back to top |
|
|
zaratystra
|
| Joined: 16 Feb 2005 |
| Posts: 36 |
|
1656.40 Points
|
|
|
Carfentanil
Wed Feb 16, 2005 6:25 pm |
|
|
| Carfentanil is 10 000x more potent for morfine |
|
| Back to top |
|
|
stooge
|
| Joined: 11 Feb 2005 |
| Posts: 56 |
|
1401.36 Points
|
|
|
Thu Feb 17, 2005 2:41 pm |
|
|
as far as i understood you maybe meant if there is any kind of fentanlys to be synthesized from tempidone? at least that's what i'd be interested in  |
|
| Back to top |
|
|
Klot
|
| Joined: 14 Feb 2005 |
| Posts: 93 |
|
581.06 Points
|
|
|
Thu Feb 17, 2005 2:46 pm |
|
|
| Quote: |
|
ar as i understood you maybe meant if there is any kind of fentanlys to be synthesized from tempidone? at least that's what i'd be interested in
|
Yes i asked information for activity fentanyl analog was to be synthesized from tempidone
2,2,6,6 tetramethyl fentanyl |
|
| Back to top |
|
|
stooge
|
| Joined: 11 Feb 2005 |
| Posts: 56 |
|
1401.36 Points
|
|
|
Thu Feb 17, 2005 5:06 pm |
|
|
very interesting indeed - i wonder about the legality of tempidone in the EU as every information to be found is only from bulgaria and russia. would be no problem to order online, but it seems to be a little of a hazard without knowing if one's going to have trouble ordering a possibly scheduled substance ...
no clue how to find out ... |
|
| Back to top |
|
|
Klot
|
| Joined: 14 Feb 2005 |
| Posts: 93 |
|
581.06 Points
|
|
|
Thu Feb 17, 2005 5:11 pm |
|
|
tempidone may be easy to synth
patent
US 4,536,581 |
|
| Back to top |
|
|
zaratystra
|
| Joined: 16 Feb 2005 |
| Posts: 36 |
|
1656.40 Points
|
|
|
Thu Feb 17, 2005 6:06 pm |
|
|
tempidone may be VERI easy to synth ...
acetone and CaCl2 (angidride) + NH3 |
|
| Back to top |
|
|
Willie
|
| Joined: 14 Feb 2005 |
| Posts: 75 |
| Location: Moscow |
1107.76 Points
|
|
|
Thu Feb 17, 2005 7:30 pm |
|
|
It's almost clear with raw material: it can be purchased j synthezed. Âut what's to do next?
Does anybody know the suitable OTC way? |
|
| Back to top |
|
|
stooge
|
| Joined: 11 Feb 2005 |
| Posts: 56 |
|
1401.36 Points
|
|
|
Fri Feb 18, 2005 1:25 am |
|
|
cool!
acetone and CaCl2 (angidride) + NH3
But could you give a little more detailed description for the more dumb around here, err, like, say, me ... 
everything i could find out yet on tempidone is, that it's said to be anxiolytic, calming and (?) anaestethic, so it's very interesting!
anyone knows more on that? |
|
| Back to top |
|
|
|
|
|
Fri Feb 18, 2005 10:14 am |
|
|
Great,
What is the route then from tempidone to such a powerful Fentanyl,?
Just looking at the Patent now,..
My god, that is a great patent,
It looks alot like the proposed Piperidone synthesis, mannich style,
Wow, I have searched for along time, for this patent
This is Big news
So I guess the next question is on the synthesis from tempidone to a more active Opiate,.
syn |
|
| Back to top |
|
|
Klot
|
| Joined: 14 Feb 2005 |
| Posts: 93 |
|
581.06 Points
|
|
|
Fri Feb 18, 2005 12:56 pm |
|
|
| Quote: |
|
everything i could find out yet on tempidone is, that it's said to be anxiolytic, calming and (?) anaestethic, so it's very interesting!
|
i have a referens on paper for tempidon activity , but i have not a full text for this paper
may anybody have it ?
Acta Physiol Pharmacol Bulg. 1974;2:76-81.
Pharmacological studies of some central effects of tempidon.
Georgiev V, Petkova B.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=4157111
Agressologie. 1975;16 Spec No C:43-7.
Study of development of tolerance to and barbiturate-like physical dependence on the tranquilizer tempidon.
Nikolova M, Daleva L, Nikolov R.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=1241886
Neuropharmacology. 1972 Nov;11(6):801-5.
An attempt to elucidate the central depressive action of Tempidon.
Daleva L, Nikolova M.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=4404708
Eksp Med Morfol. 1979;18(1):5-12.
[Pharmacokinetics of the original Bulgarian preparation, tempidon, in experimental animals]
[Article in Bulgarian]
Mikhailova D, Ognianova V, Chobanova I.
The authors carried out a pharmacokynetic study on the Bulgarian preparation Tempidone in rats. They examined resorption, distribution and excretion of the preparation in urine, bile and feces of rat after venous and oral administration. The experiments were carried out on 207 white male rats of the Wistar strain, weighting from 160 to 180 gm. Blood samples were obtained at various intervals from the onset of venous administration of the preparation in a dose of 100 mg/kg of body weight. After oral administration of the dose of 125 mg/kg of body weight in addition to blood samples other samples from brain, liver, stomach and intestines (small and large) were obtained as well. Excretion of Tempidone through the bile was examined after intraperitoneal administration of 250 mg/kg of body weight. They proposed pharmakynetic models after venous and oral administration of Tempidone. The obtained results gave evaluation for the rate, with which the distribution processes in the organism of rats occurred. Pharmacologic action of Tempidone coinceded in time with the creation and support of effective plasma concentrations. The wide distribution and preservation of Tempidone in the tissues suggested that it underwent the so called tissue binding.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=436713 |
|
| Back to top |
|
|
stooge
|
| Joined: 11 Feb 2005 |
| Posts: 56 |
|
1401.36 Points
|
|
|
Sat Feb 19, 2005 12:24 am |
|
|
hey klot, synthetika, very cool :)
this sounds even somehow more mac-gyveresk than the old i2/rp ---- method:)
Now, swim never used an autoclav, no clue at all - if one was using a normal steam presure cooker for this, could he just put the mixture in it in an open vessel, close the lid of the pot and use it like that? with working in an thermometer into that apparatus somehow, and so on? i guess that should work, or ... err ...? |
|
| Back to top |
|
|
THE MOON RULES --1
voted for the moon
|
| Joined: 24 Feb 2005 |
| Posts: 35 |
| Location: Police State |
238.62 Points
|
|
|
Thu Feb 24, 2005 12:45 pm |
|
|
| erased |
|
| Back to top |
|
|
longimanus
|
| Joined: 08 Aug 2005 |
| Posts: 5 |
|
283.24 Points
|
|
|
Tempalgin and its friends
Mon Aug 08, 2005 11:44 pm |
|
|
So long waiting and finally someone gets tempidone seriously. And especially its role as a starting material for fentanyl analogues.
Well, first of all tempidone is no longer manufactured as the 30 mg tablets, now it`s available only as a combination with analgin (methansulfonic acid sodium salt) - Tempalgin, 10 film-tabs for 1.80 levs or ~ $1.20. Suppose it`s not manufactured since the big unreregistration of drugs (~1200 in number, as much as I remember) in the beginning of the century. Tempidone is mainly refered as a CNS depresant and neuromuscular blocker and is known to boost the effects of depressants and analgetics (nice feature if one has only one tablet of phenazepam). And, last but not least, Tempalgin, together with codeine and ergotamine and their combinations with caffeine, is capable of dulling my headache (VIVA!).
Oh, and I forgot to mention, if one is thinking of bying triacetonamine (another name of tempidone) from some vendor, well, let this one reassure him/herself of his/her ability to waste lots of money for almost nothing. In this context I think you will be happy to know that there is a patent BG63941 for the production of tempidone from 2001 (as much as I know - the most recent) that does not require
| Quote: |
|
acetone:ammonia molar ratio of 20:1 to 4:1
|
and
| Quote: |
|
pressure of 1 to 50 atmospheres
|
as the procedure in US4536581. Possibly the problem for you would be that it`s in Bulgarian but ... what am I here for? I`m not telling that I`ll translate the whole patent (if someone buys me a beer or two I`ll think about it  ) but what about the significant part:
A. Production of acetonine
1.5 mol acetone are loaded in RB flask equipped with barboteor (or барботьор - studing medicine, not chemistry )and 0.1 mol catalyst are added. The reaction mixture is cooled to -10degC and saturated with gaseous ammonia for 6h. After that the temperature is allowed slowly to rise to room temperature at which the mixture stays 10-16h. The resulting product is analysed through GC and without any further processing is used for the next stage of the synthesis.
Catalyst - Yield- Conc. hydrochloric acid (37%) - 92%
- Ammonium chloride - 86%
- Ammonium bromide - 96%
B. Production of triacetonamine
The produced by the above method acetonine is diluted additionally with acetone, siccative and catalyst are added and the mixture is stirred from 10 to 24h at room temperature.
Example(#) - Acetone(mols) - Catalyst(mols) - Siccative(chemical name) - Siccative(mols) - Time(h)- 1 - 20 - 1.76 - magnesium sulfate - 0.9 - 20
- 2 - 8.7 - 1.30 - magnesium sulfate - 0.9 - 20
- 3 - 38 - 2.47 - sodium sulfate - 0.56 - 24
- 4 - 27 - 1.76 - calcium oxide - 0.8 - 16
- 5 - 25 - 1.6 - sodium sulfate - 0.45 - 25
- 6 - 15 - 2.0 - calcium chloride - 1.0 - 24
- 7 - 27 - 1.76 - sodium sulfate - 0.4 - 24
As catalyst in every one of the examples could be used: methanol, saturated with hydrogen chloride, chloroacetic acid, chlorosulfonic acid, ammonium chloride, ammonium bromide, ammonium p-toluensulfonate.
C. Production of p-toluensulfonic salt of triacetonamine
Solution of 1 mol triacetonamine, afforded through one of the methods above, is cooled to temperature of 0-5degC. The amount of triacetonamine is determined with GC. To the coold solution is added dropwise solution of 1g p-toluensulfonic acid in acetone untill the quantity of p-toluensulfonic acid reaches 1-1.3 mol per mol triacetonamine. The end of the process is determined when pH of the reaction mixture reaches 5. The produced precipitate is filtered, washed with acetone and dried at temperature of 60degC.
Yield of the p-toluensulfonic salt 70-80%towards the amount of triacetonamine.
Sorry, about the fomat and possible mistakes in the translation but it was created on-the-fly and I hope I`ll be forgiven.
And at the final, again about that fentanyl analogue. According to my view of the things the replacement of piperid-4-one with tempidone will result in a compound with characteristics, similar to these of alpha-methylfentanyl - this could be easily illustrated with every one 3D-molecular-structures-creating program. These four methyl groups around the piperidine nitrogen did not attenuated the ability for hydrogen bond formation of the atom - results from a calculation of mine, performed about a year ago. Further modifications of the molecule would possibly produce even more interesting results - for example ohmefentanyl or carfentanyl analogues. |
|
| Back to top |
|
|
|
|
|
Powered by phpBB 2.0.11 © 2001, 2002 phpBB Group
Igloo Theme Version 1.0 :: Created By: Andrew Charron
|
Forums
Rhodium
The Hive
Shop
Profile
Log in
Register
Log in to check your private messages
474