N&PD Moderators: Skorpio
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Smyth2
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4DQSAR
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I also find the chemistry sort of dull. Once you have seen a few clandestine labs, you quickly decide that no, you don't want to put ANYTHING made that way into your body.
I like opioid chemistry BECAUSE nobody has been able to find a set of rules. It's a genuine unknown where an independant researcher can genuinely improve upon that which is known. But I don't go anywhere NEAR breaking the law, ever.Smyth2
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1-[4-Fluoro-3-(trifluoromethyl)phenyl]propan-2-amine
pubchem.ncbi.nlm.nih.gov
1-[3-Fluoro-4-(trifluoromethyl)phenyl]propan-2-amine
pubchem.ncbi.nlm.nih.gov
Smyth2
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Eckard Weber, John Keana, & Peter Barmettler, WO1990012575 (Oregon State Board of Higher Education, Oregon State).
Gee KR, Barmettler P, Rhodes MR, McBurney RN, Reddy NL, Hu LY, Cotter RE, Hamilton PN, Weber E, Keana JF. 10,5-(Iminomethano)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene and derivatives. Potent PCP receptor ligands. J Med Chem. 1993 Jul 9;36(14):1938-46. doi: 10.1021/jm00066a002. PMID: 8101572.
It shares the same precursor that is used to make Diphenidine, namely 1,2-diphenylethylamine.4DQSAR
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They EVEN had the cheek to say 'oh, we can't make the N-isopropyl because of the low BP of the amine'. So I sent a RT route with quantitative yields and methanol as solvent... and they STILL tried to tell the boss they couldn't make it...
Funny - the boss sacked them quite soon afterwards. If I take a man's dollar, I work to make the man money. The labrats were only interested in their own cut. Understandable - But don't take a banana to a knife-fight if you intend to argue facile syntheses.
I ASSUME these compounds to be more potent - but I can make isophendine for about £400/Kg - see also 'very facile indeed'.Smyth2
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BRN 2382808
11-Dimethylamino-9,10-dihydro-9,10-ethanoanthracene
[4053-11-6]
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DE1291743 idem Herbert Schroter & Daniel A Prins, US3519718 (1970 to Novartis Corp).
Boissier JR, Ratouis R, Dumont C, Taliani L, Forest J. Synthesis and pharmacological properties of new 9,10-dihydro-9,10-ethanoanthracene derivatives. J Med Chem. 1967 Jan;10(1):86-91. doi: 10.1021/jm00313a018. PMID: 4382229.
Herbert Schroter & Daniel A Prins, US3422104 (1969 to Novartis Corp).

Deleted member 576750
Discord Sr. Moderator
I think the opioids are likely that way because the natural ligands are polypeptides rather than small molecule transmitters
I also find the chemistry sort of dull. Once you have seen a few clandestine labs, you quickly decide that no, you don't want to put ANYTHING made that way into your body.
I like opioid chemistry BECAUSE nobody has been able to find a set of rules. It's a genuine unknown where an independant researcher can genuinely improve upon that which is known. But I don't go anywhere NEAR breaking the law, ever.
Likely other receptors that respond to endogenous polypeptides are similarSmyth2
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[1] Rajagopalan, P. (August 1984). "Synthetic CNS agents. 1. (.+-.)-1,2,3,4,4a,5,10,10a-Octahydro-5,10[1',2']-benzenobenz[g]isoquinoline hydrochloride. A new, highly potent, potential antidepressant". Journal of Medicinal Chemistry. 27 (8): 946–947. doi:10.1021/jm00374a002.
[2] Rajagopalan, P. (22 January 1985). "ChemInform Abstract: SYNTHETIC CNS AGENTS. 1. (.+-.)-1,2,3,4,4A,5,10,10A-OCTAHYDRO-5,10(1′,2′)-BENZENOBENZ(G)ISOQUINOLINE HYDROCHLORIDE. A NEW, HIGHLY POTENT, POTENTIAL ANTIDEPRESSANT". Chemischer Informationsdienst. 16 (3). doi:10.1002/chin.198503229.
[3] Parthasarathi Rajagopalan, US4351836 (1982 to Bristol Myers Squibb Pharma Co).
[4] Zhang Hui, CN101696187 (2011 to Xuzhou College of Industrial Technology).