Substituted phenylmorpholine Class of chemical compounds
Substituted phenylmorpholines , or substituted phenmetrazines alternatively, are chemical derivatives of phenylmorpholine or of the psychostimulant drug phenmetrazine . Most such compounds act as releasers of monoamine neurotransmitters, and have stimulant effects. Some also act as agonists at serotonin receptors, and compounds with an N-propyl substitution act as dopamine receptor agonists . A number of derivatives from this class have been investigated for medical applications, such as for use as anorectics or medications for the treatment of ADHD . Some compounds have also become subject to illicit use as designer drugs .[ 1] [ 2] [ 3] [ 4]
Various phenmetrazine derivatives
The 2S,3S isomer of phendimetrazine (i.e. (2S,3S)-3,4-dimethyl-2-phenylmorpholine)
The (+)-enantiomer & (−)-enantiomer of pseudophenmetrazine .
List of phenmetrazine analogues and related compounds
Substance
Structure
CAS number
2-phenylmorpholine
23972-41-0
2-phenyl-3-methylmorpholine (phenmetrazine)
134-49-6
2-phenyl-3,4-dimethylmorpholine (phendimetrazine )
634-03-7
2-phenyl-5-methylmorpholine (isophenmetrazine)
80123-66-6
2-phenyl-3-ethylmorpholine (phenetrazine)
100368-98-7
2-phenyl-3-methyl-4-ethylmorpholine (phenmetetrazine)
92196-09-3
2-phenyl-3,5-dimethylmorpholine (PDM-35 )
1218345-44-8
2-phenyl-3,6-dimethylmorpholine (6-methylphenmetrazine, 3,6-DMPM)
92902-99-3
2-phenyl-5,5-dimethylmorpholine (G-130 )
42013-48-9
2-phenyl-3-methylmorpholin-5-one (fenmetramide )
5588-29-4
4-isopropyl-2-phenylmorpholine[ 5]
23222-62-0
Fenbutrazate
4378-36-3
Morazone
6536-18-1
2-Fluorophenmetrazine
1533654-24-8
3-fluorophenmetrazine (PAL-593)
1350768-28-3
4-Fluorophenmetrazine (PAL-748)
1097796-73-0
3-fluorophenetrazine
3-chlorophenmetrazine (PAL-594)
1097796-78-5
3-Methoxyphenmetrazine
2-Methylphenmetrazine
1507705-48-7
3-methylphenmetrazine (PAL-773)
1350768-41-0
4-methylphenmetrazine (PAL-747)
1998216-41-3
4-methylphendimetrazine
1445576-23-7
3,4-Methylenedioxyphenmetrazine [ 6]
Naphthylmetrazine (PAL-704)
2-(thiophen-2-yl)-3-methylmorpholine
2-(2,5-dimethoxy-4-bromophenyl)morpholine[ 7]
2-(3-(Trifluoromethyl)phenyl)morpholine (flumexadol )[ 8]
30914-89-7
Oxaflozane
26629-87-8
Phenmetrazol
1350768-19-2
N-Ethylphenmetrazol
97630-98-3
(+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethylmorpholin-2-ol (radafaxine )
106083-71-0
(2S,3S,5R)-2-(3,5-difluorophenyl)-3,5-dimethylmorpholin-2-ol (manifaxine )
135306-39-7
PF-219,061 [ 9]
710654-74-3
PF-592,379
710655-15-5
OSU-6162
156907-84-5
LPH-5 [ 10]
2641630-97-7
2-Methyl-3-phenylpiperidine
70769-67-4
2-Phenyl-3-methyl-thiomorpholine
Picilorex
62510-56-9
Butyltolylquinuclidine
3-benzylmorpholine (3-BZM)[ 11]
7684-27-7
3-Benzhydrylmorpholine (3-BZHM)
93406-27-0
See also
References
^ Boswell GE (1997). "Synthesis, stereochemistry and anti-tetrabenazine activity of bicyclo analogues of 2-phenylmorpholines" . Journal of Heterocyclic Chemistry . 34 (6): 1813–1820. doi :10.1002/jhet.5570340629 .
^ US 20130203752 , Blough BE, Rothman R, Landavazo A, Page KM, Decker AM, "Phenylmorpholines and analogues thereof", published 8 August 2013
^ Mayer FP, Burchardt NV, Decker AM, Partilla JS, Li Y, McLaughlin G, et al. (May 2018). "Fluorinated phenmetrazine "legal highs" act as substrates for high-affinity monoamine transporters of the SLC6 family" . Neuropharmacology . 134 (Pt A): 149–157. doi :10.1016/j.neuropharm.2017.10.006 . PMC 7294773 . PMID 28988906 .
^ McLaughlin G, Baumann MH, Kavanagh PV, Morris N, Power JD, Dowling G, et al. (September 2018). "Synthesis, analytical characterization, and monoamine transporter activity of the new psychoactive substance 4-methylphenmetrazine (4-MPM), with differentiation from its ortho- and meta- positional isomers" . Drug Testing and Analysis . 10 (9): 1404–1416. doi :10.1002/dta.2396 . PMC 7316143 . PMID 29673128 .
^ Chem-Sink (chemicals that are Sn2 products & Friedel-Crafts alkylation reactants)
^ Swist M, Wilamowski J, Zuba D, Kochana J, Parczewski A (May 2005). "Determination of synthesis route of 1-(3,4-methylenedioxyphenyl)-2-propanone (MDP-2-P) based on impurity profiles of MDMA". Forensic Science International . 149 (2–3): 181–92. doi :10.1016/j.forsciint.2004.06.016 . PMID 15749360 .
^ Glennon RA, Bondarev ML, Khorana N, Young R, May JA, Hellberg MR, et al. (November 2004). "Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane". Journal of Medicinal Chemistry . 47 (24): 6034–41. doi :10.1021/jm040082s . PMID 15537358 .
^ Chemicalbook dot com: Flumexadol
^ Morpholine Dopamine Agonists For The Treatment Of Pain. Michael Andrew Ackley US 2009/0318451 AI Dec., 24th 2009. 1st Page.
^ Kristensen J, et al. 5-HT2A Agonists for Use in Treatment of Depression. Patent US 2021/0137908
^ NIH PubChem Compound Summary for CID 3283983
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