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Daniel Lednicer

Well, that'a a good start, so thank you for that. Anyone have newer info. This guy looks like an overlooked genius. I notice Gruenthal are trying to make a patent on on his super-opiates (see US Patent 7,183,436). Even their route is a bit more tortourous than his (lower yielding as well).
 
Zoominfo

Published on: 3/13/1999 Last Visited: 8/12/2001
Daniel Lednicer , Ph.D. B.S. Antioch College ; Ph.D. , Ohio State University ; Postdoctoral Fellow at Duke University. Dr. Lednicer has experience at G. D. Searle , Upjohn Co. , Mead Johnson & Co. , and Adria Laboratories. He was NIH Project Officer for synthesis of anti-tumor compounds and anti-HIV compounds and manufacture of dosage forms for clinical studies. Editor and Chapter author on numerous books on medicinal chemistry ; co-author of the first four volumes and sole author of the most recent volume of the well known series The Organic Chemistry of Drug Synthesis. Numerous positions with the American Chemical Society Division of Medicinal Chemistry , including Division Chairman and Scientific Program Chairman for the 16th national symposium. Authored more than 70 peer-refereed papers and invented more than 65 U.S. patents. He actively participates in new drug development at DTI and is a co-inventor on DTI's most recent patent.
Click to expand...
 
Also, in addition to some of his earlier ebooks, it appears as though there is some more recently published books by this mysterious guy who seemingly prefers to keep his identity anonymous.
 
I've found an old email address for him here: Pubmed.

Pubmed (or another journal article database) is a good way of contacting academic researchers - they'll usually list their email address, or the university they work at. I just did a search on Lednicer, and the article I've linked to was the most recent result (from 2002). (Pubmed is a good choice because it's free and online).
 
Wow, an address I will cherish but almost certainly never use. All we need to complete the picture is that 'Eyes of God' AKA 'Nuklear' E-mailing him with his 'I am god, all praise me' attitude!
 
There's a good chance of it being treated as junk mail when u send to those prestigious professor dudes. I've certainly had few replies from them in the past although ive had a couple of interesting phone calls to Kozikowski.

What I was interested in, if these compounds are so profusely active then why hasn't their use been more closely considered?

It's good that u discovered the recent patents, although before that it appeared almost as though 'Bromadol' and friends had been abandoned.

Like, you said these compounds are delta agonists as well as mu agonists. Where's the proof of that? Nothing that I can see details the pharmacology.
 
I noticed in the patent (the rip-off German one) that the drug Bromadol should be administered with a strong opiate? que? I also noted that they suggest as the protecting group for the 1,4 hexanedione a 'hemiacetal'.... don't they mean a hemiketal? Am I missing some thing(s) here?

The Chinese changed the phenylethyl for 2-thiophen-2-yl-ethyl grouping, here but potency seems to vary hugely by species...
 
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Hemi = half

A hemiacetal usually refers to when the reaction is half complete, if you look at the mechanism for forming a cyclic acetal, which is a common part of the syllabus in undergraduate organic theory, it proceeds in 2 stages.

Acetal is used for most things, inotherwords a ketal is sometimes (wrongly) referred to as an acetal.

Moreover, you can use ethanol to make 'acetals', clearly here though 2 molar equivalents are necessary, not including the molar excess that is commonly employed.

Cyclic acetals have the advantage that they are more stable to degradation, since if one comes off, its not totally lost. So they have a more -ve Gibbs energy of formation or some such BS.

In the case of 4-piperidone though, the ethylene-ketal is so stable that it actually problematic to remove.
 
Happily Dan (aka Daniel) Lednicer is alive and well in North Bethesda, Maryland, USA. After retiring from the National Cancer Institute in 1995 i stayed in touch with chemistry by continuing to publish books: "The Organic Chemistry of Drug Synthesis" Voulme 6 (1999), Volume 7, published by Wiley just this past fall, "Strategies for Organic Drug Synthesis and Design" (1998) and "New Drug Synthesis and Development" (2006). This last book is a more general volume intended for the informed lay person that gives the history of the development of important classes of drugs.
The bios that have appeared in some of the posts which seem to come from book cover blurbs are generally correct if a bit sketchy. I will keep looking at Bluelight sinece I will be happy to engage in conversations on various topics.

Dan Lednicer
[email protected]
 
Thanks for replying to this, Dan. While I dont doubt this you, forgive my initial reservations on believing you.

I guess what im interested in, is whether 'bromadol' is suitable for human consumption, or if it feels too weird/strange.

Did you think of a pet-name of your own to call that chem?
I just made bromadol up myself, but the rights are clearly with the inventor to pick names.

We have established it is a mixed mu/delta agonist. I wonder how this feels different to a 'clean' mu agonist?

I'm certainly interested in this chem & have read quite a few of your books.

It would certainly not be first on my hit-list since the extreme potency is more of a deterrant than an attraction.

Especially with the amateur due to danger. I'm thinking when it was first discovered the world wasnt 'ready' for it.

I'm also thinking this will change over time and nothing is set in stone.

At least with bromadol, the chem is completely unique whereas fent analogs are just variations on the same theme.
 
Here is an article for people interested in learning about antidepressant DOR agonists.

I'll sit down and read a printed version myself eather than babbling too much before using brain, instead of afterwards.

In the words of Dr.Heckyll (an ADD celebrity): "DOR agonists are hardcore antidepressants."

It also follows that these will become promptly illegalized if their use spreads.
 
"Bromadol"

By "Bromadol", I assume that you refer to the hellishly potent compound 1 in our original 1979 Comminication to the Editor" in J.Med.Chem.. The answer to your question will unfortunally on necesity stay in limbo because Upjohn never expressed any interest in following up on this compound. The only one examined in any detail was one that showed mixed agonist activity...they walked away from the series when that compound showed some weird tox in chronic tests. No details since I was long gone from Kalamzoo by then.
In reply to posts on the sterochemistry, the same paper noted above shows a conformation of "bromadol" that provides a perfect overlay with fentanyl. There is some more speculation on that at the end of my chapter in "Central Analgetics".

As to establishing my bona fides...? Googling me will only confuse you as an early hit will be a Website that displays miniature pastel paintings http://dan.lednicer.com. That represents a secondary career that I took up on retirement.

Dan
 
If I may ask, is Bluelight a site you had frequented in the past? Or did you join after (what I presume was) an awkward self-google?

I imagine I'd feel a little awkward if I found a whole thread devoted to me (actually, this is the second you've gotten in recent weeks, congrats! ;) )
 
welcome to BL
FWIW I think the organic chemistry of drug synthesis is a great series of books, a wide ranging backgrounder series.
I should add volume 7 to the collection at some point.
 
Googling

You must admit that "Who is Daniel Lednicer?" is a rather attention-grabbing hit!!
 
I'd imagine it would be odd... Around here, though, people in your area are revered. Now you're famous!

edit: Since it was being discussed in another thread, and you'd likely have first hand knowledge, could you comment on how common "accidental ingestion" is for those researching psychoactives?
 
Please... do not scare the man away with questions like that. Do you really expect an answer?
 
If you read the MOTM under etorphine it can be seen that this has happened and can be actually very dangerous. More famously, it occured with Hoffman and LSD-25 but clearly its an issue with drugs active in micrograms, not milligrams.

Etorphine is another of my personal favorites, less so for PPOM. These semi-synthetics nuke out mu/delta/kappa receptors. Kappa isnt really meant to be desirable but an expert in this area said that to an addict, it may not be that undesirable to trip slightly, and could add to the high. People will intentionally take Salvia A, so its not like this is inconceivable. Also remember Herkinorin brought up a while ago? At first I rejected it since there are 3 ester groups that can be hydrolyzed in Salvia A: acetyl, methyl ester, and cyclic lactone. However, after seeing it recently, although I dont have the literature to back it up, yet, I think it looks very elegant molecule and find it inspirational.
 
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lol!

they actually listened to me
 
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Quick question.... what is the onset of 'Bromidol'? The patents mention giving the drug WITH a strong opiate agonist, so I'm a little confused (as usual)..
 
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