Any Propositions for Exciting, New, Novel Benzos or Analogs??

[parcival]

It does have the 1-4 diazepine ring that is fused with a benzene, essentially the core of the benzodiazepines, and has a weak interaction at the GABA1 site. It even came out of the SAR search for sulphur containing BDP and belongs to the group of the thienobenzodiazepines just like brotizolam
clotiazepam and etizolam. Its use as an antipsychotic instead of a anxiolitic has to do with its different receptor profile.

 

[Hammilton]

olanzapine is a 1,5-benzodiazepine, not a 1,4.

It even came out of the SAR search for sulphur containing BDP and belongs to the group of the thienobenzodiazepines just like brotizolam
clotiazepam and etizolam.

I assume that BDP is a mistake for BZP.

Anyway, that claim doesn't seem to be true. Olanzapine was discovered as an analogue of the much older clozapine, of which it is a simple analogue, not in some sort of "SAR search for sulfur-containing benzodiazepines." As you mention, there are old and well characterized sulfurous benzos that have been marketed for a long time. Olanzapine is relatively new compared to any benzos marketed in the US (it's been a long time since a new one has been brought to market)

 

[Holy_cow]

There was that benzo that supposedly mimiced the effects of alcohol. Anyone remember the name?

 

[/navarone/]

QH-ii-066
A highly selective GABAa alpha-5 subtype agonist supposively responsable the anxiolitic/sedative/euphoric effects of ethanol.

SH-053-R-CH3-2′F also holds the title of a strong selective alpha-5 agonist although slightly different from the former.
(Interestingly, it shares some similiarities with imidazenyl and it has an alpha methyl group preventing hepatic alpha hydroxylation, like meclonazepam)

Anyway has anyone else tried (Triazolo)thienodiazepines?

I'm undecided between taking clotiazepam (a simple thienodiazepine with short HL, 4-6h, medium potency, ~10mg, but high peak, 1.5h) and etizolam (a triazolothienodiazepine with longer HL, 6-10h, higher potency, ~3mg, slower peak, 3h, but considering that triazolobenzodiazepines normaly give me strong amnesia and knockout effects).

 

[Holy_cow]

^That's it, thanks a lot!

 

[dread]

Olanzapine lacks the phenyl group of actual benzodiazepines, therefore I personally would not classify it as a benzodiazepine, although it does contain a benzodiazepine moiety

 

[/navarone/]

How come they never made a triazobenzodiazepine analogue flunitrazepam? Or something like nitro midazolam?

:drools:

 

[dread]

I've also thought about it, a nitro-analogue of midazolam would probably kick ass. OTOH though, it would also probably be amnesic as fuck.

(seriously... midazolam & flunitrazepam, two of the most amnesic benzos known, and you wanna cross-breed them??? are you trying to forget something? )

 

[seep]

How come they never made a triazobenzodiazepine analogue flunitrazepam? Or something like nitro midazolam?

This:

is dealt with in 18 patents.




Flunitromidazolam (or whatever you wanna call it, as the orthofluorophenyl is implied in the "midazolam" part): no exact match. Preserving the 1-methylimidazole (which seems to be the optimal spot for the methyl subtituent), you have USP#3933794:

which is 3H instead of 4H on the imidazole.



If you must preserve the 1-methyl-4H-imidazobenzodiazepine structure, you have to settle for the intermediate in USP#4368157, 4368158 and 4368159:

and finish the synthesis.

 

[/navarone/]

I've also thought about it, a nitro-analogue of midazolam would probably kick ass. OTOH though, it would also probably be amnesic as fuck.

(seriously... midazolam & flunitrazepam, two of the most amnesic benzos known, and you wanna cross-breed them??? are you trying to forget something? )

And short acting like an orgasm probably

Ah btw I finaly managed to try IV midazolam (twice) .

As I wrote way back in this thread, midazolamis is not sold in the Italian pharmaceutical market, it used excluselively in hospital institutions for prenestetizing patients during an operation.

So well, you can guess navarone has been sick....very sick, hospitalized 16 days for a tremendous flebitis with muscle infection and luclkily didn't get his arm amputated (always sterylise thoroughly your equipment guys...neva know which evil germ is waiting ro suck your blood).

This is the scenario:
well now I was already on the operation table ready for intervention and the Surgeon injects me with something:

Me: (curious)What are you giving me?
Surgeon: It is just something to calm you down...
Me: Midazolam?
Surgeon: (surprised)..ehh...yes.
Me: (smiling) Good Shit!
Surgeon: What?

 

[seep]

is dealt with in 18 patents.

Jesus, these are Hoffman-LaRoche lab manuals for the full synthesis of thousands of imidazobenzodiazepines.

 

[/navarone/]

Not so surprising afterall.
Syntheses of the researched compound are usually inclued in theese papers. Even if you look on wikipedia or google yuo can find the synthesis for VX (the most lethal exsting nerve agent and the syntesis of sarin which is quite simple and does'nt tequire a big chemist nor complex chemicals)

Still do u think that yu'll be able to cook theese benzos in your kitcen?..I guess not!
Even all of the black maket pharms/benzos come mostly from chinese from serioul laboratories.

It would be cool though to extract/puify an existing benzo change it abit with some chemestly.

Someone here manged to methylate clonazepam (clonitrazepam) stating that it was more potent than the former.
A triazolobenzodiazepine version of clonazepam shouldnt be so difficul to make either.

 

[/navarone/]

This:

is dealt with in 18 patents.




Flunitromidazolam (or whatever you wanna call it, as the orthofluorophenyl is implied in the "midazolam" part): no exact match. Preserving the 1-methylimidazole (which seems to be the optimal spot for the methyl subtituent), you have USP#3933794:

which is 3H instead of 4H on the imidazole.



If you must preserve the 1-methyl-4H-imidazobenzodiazepine structure, you have to settle for the intermediate in USP#4368157, 4368158 and 4368159:

and finish the synthesis.

BTW seep, your final benzo caught my attention, I don't quite get the ethyl on the 4' position, is it to block the enzymatic action of P450?

Do you have any other info onthe benzos you listed above, i'm so curious!
It would be greatly apreciated!

 

[dread]

Ah btw I finaly managed to try IV midazolam (twice) .

Didya like it?

 

[seep]

Someone here manged to methylate clonazepam (clonitrazepam) stating that it was more potent than the former.

Because first-pass metabolism will attack the amine before the nitro, I think.

Do you have any other info onthe benzos you listed above, i'm so curious!

Others may have a more efficient way. What I did was register (free) at http://www.patentstorm.us/ and then search by patent number. That'll let you download the patents as pdfs.

 

[/navarone/]

Didya like it?

Well, i was practically naked on an operation table with a big fashing light over my head withpulse meters all'over my body and about to have my completely swollen and muscularly infected arm cut into pieces to get rid of 200ml of pus.

Apart from that...yeah it was Keelw!!!

The doctors where surpised how how exited i was after the operation.

 

[daddysgone]

Well, i was practically naked on an operation table with a big fashing light over my head withpulse meters all'over my body and about to have my completely swollen and muscularly infected arm cut into pieces to get rid of 200ml of pus.

Apart from that...yeah it was Keelw!!!

The doctors where surpised how how exited i was after the operation.

Off topic, but what put you in the hospital? You mentioned phlebitis, but didnt mention how you managed to get it? Non-sterile IV practice? Glad to hear you are better now.-DG

 

[dread]

I wager it was injection that missed a vein. In the past I've done some unsanitary IV injections and had a hard time getting an infection, but if the injection misses the vein... that's a different story.

Although non-sterile IM injections are the worst.

 

[/navarone/]

Yep it was an injection. Boy you can't imagine how stupid i felt those days in the hospital looking at the arm i fucked up.

Anyway back on topic i had an idea of a benzo that i guess could be easily made from Clonazepam.

"Triazolo-clonazolam" or nitro-triazolam.
turning the ketone into an imine and then bla bla bla should't be so difficult.

 

[DILAUDID 8mg]

I'd like to mention two points. The triazolo-benzodiazepines (the one's the end in LAM) are not that much different than their cousins whose names end in pam. The biggest difference is the relative potency mg for mg and the normal elimination half-lives of the two classes. The triazolo-analogues generally have a shorter half-life, thus duration of action. The problem I have with these are that the rebound anxiety is quite often worse than the baseline anxiety levels in most patients, which is counter-productive. Second, everyone reacts differently to the same chemicals.