N-(1-phenylcyclohexyl)piperidine [PCP]

Page 1

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PubChem

eMolecules

Reactions (16)

Yield

Substances (5)

Conditions

Citations (21)

References

1

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Rx-ID: 2735991 Find similar reactions

73%

2

in diethyl ether; benzene

T=20°C;

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Katritzky, Alan R.; Najzarek, Zbigniew; Dega-Szafran, Zofia

Synthesis, 1989 , # 1 p. 66 - 69 Title/Abstract Full Text Show Details

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Rx-ID: 6458498 Find similar reactions

Union Carbide Chemicals and Plastics Technology Corporation

Patent: US5302767 A1, 1994 ; Title/Abstract Full Text Show Details

3:PCP Preparation with Air Atmosphere

EXAMPLE 3 PCP Preparation with Air Atmosphere 326 g of DMSO was heated to 85° C. in a 1 l baffled, glass resin kettle. 160 g of 50 weight percent aqueous sodium hydroxide was added, and the reactor contents were allowed to return to 85° C. 120 g of 50 weight percent aqueous Q-salt solution, as prepared in accordance with Example 1, was added over a period of 1 minute. The reactor contents were then maintained at 85° C. for a further 25 hours. Throughout this period, the reaction mixture was left exposed to the air. At the end of the reaction period, finely dispersed, off-white solids had formed. These were collected by filtration, washed with water, and then refluxed in 400 ml toluene for 60 minutes. The resulting solution was filtered while still hot to remove the undissolved polymer. The toluene was allowed to cool and the resulting crystals were recovered by filtration. A second crop of crystals was taken by stripping toluene, allowing the remaining solution to cool and recovering the resulting crystals by filtration. The resulting solids were washed with acetone and dried in an oven, yielding 15.3 g of PCP (51percent yield) as white crystals. 0.6 g (2.0percent yield) of polymer were recovered. 37%

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Union Carbide Chemicals and Plastics Technology Corporation

Patent: US5302767 A1, 1994 ; Title/Abstract Full Text Show Details

C.A:PCP Preparation with Nitrogen COMPARATIVE EXAMPLE A PCP Preparation with Nitrogen 326 g of DMSO was heated to 85° C. in a 1 liter (1) baffled, glass resin kettle. 160 g of 50 weight percent aqueous sodium hydroxide was added, and the reactor contents allowed to return to 85° C. 120 g of 50 weight percent aqueous Q-salt solution, as prepared in accordance with Example 1, was added over a period of 1 minutes. The reactor contents were then maintained at 85° C. for a further 25 hours. Throughout this period, a nitrogen atmosphere was maintained over the reaction mixture. At the end of the reaction period, finely dispersed, off-white solids had formed. These were collected by filtration, washed with water, and then refluxed in 400 milliliters (ml) toluene for 60 minutes. The resulting solution was filtered while still hot to remove the undissolved polymer. The toluene was allowed to cool and the resulting crystals were recovered by filtration. A second crop of crystals was taken by stripping toluene, allowing the remaining solution to cool and recovering the resulting crystals by filtration. The resulting solids were washed with acetone and dried in an oven, yielding 11.7 g of PCP (37percent yield) as white crystals. 3.0 g (9.6percent yield) of polymer were recovered. 25.8%

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Union Carbide Chemicals and Plastics Technology Corporation

Patent: US5302767 A1, 1994 ; Title/Abstract Full Text Show Details

4:PCP Preparation with Air Sparge

EXAMPLE 4 PCP Preparation with Air Sparge 3848 g of DMSO were heated to 85° C. in a 12 l stirred tank reactor. 960 g sodium hydroxide pellets, 810 g of distilled water and 1600 g of 42.3 weight percent aqueous Q-salt solution, prepared in accordance with Example 1, were added. The reactor contents were then maintained at 85° C. for a further 4 hours. Throughout this period, the reaction mixture was sparged with air at a flow rate of 400 ml per minute. 91.2 g of PCP (25.8percent yield) and 3.3 g (0.9percent yield) of polymer were obtained following the recovery method described in Example A. Hide Details 1.6%

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Union Carbide Chemicals and Plastics Technology Corporation

Patent: US5302767 A1, 1994 ; Title/Abstract Full Text Show Details

5:PCP Preparation with Oxygen Sparge

EXAMPLE 5 PCP Preparation with Oxygen Sparge 42.6 kilograms (kg) of DMSO were heated to 85° C. in a 30 gallon stirred tank reactor. 21.3 kg of 50 weight percent aqueous sodium hydroxide and 15.9 kg of 50 weight percent aqueous Q-salt solution, prepared in accordance with Example 1, were added. The reactor contents were then maintained at 85° C. for a further 4 hours. Throughout this period, the reaction mixture was sparged with 2 mol percent oxygen in nitrogen mixture at a flow rate of 2 l per minute. 1347 g of solids were filtered from the reaction mixture. 150.5 g of these solids were taken for PCP recovery, following the method described in Example A. 125.2 g of PCP (28percent yield) and 7 g (1.6percent yield) of polymer were obtained.


Maddox,V.H. et al.

J. Med. Chem., 1965 , vol. 8, p. 230 - 235 Title/Abstract Full Text View citing articles Show Details

Parke; Davis and Co.

Patent: US3097136 , 1960 ; Chem.Abstr., 1963 , vol. 59, # 13881 Full Text Show Details

Mousseron et al.

Chimica Therapeutica, 1966 , vol. 1, p. 284,286 Full Text Show Details

Sokolovsky; Hordeckai

Patent: DE2339342 , 1974 ; Chem.Abstr., vol. 80, # 132908 Full Text Show Details

Parke; Davis

Patent: US3192219 , 1965 ; Chem.Abstr., 1965 , vol. 63, # 9921f Full Text Show Details

Welvart

Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences, 1960 , vol. 250, p. 1870,1871 Full Text Show Details

Kalir et al.

European Journal of Medicinal Chemistry, 1978 , vol. 13, p. 17,18 Full Text Show Details

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University of Pittsburgh

Patent: US5132313 A1, 1992 ; Title/Abstract Full Text Show Details

Compounds 3 and 4

Compounds 3 and 4 A solution of 150 mg (0.81 mmol) of compound 1 or 2 in 5.6 mL of dry ethanol was stirred with 3.8 mg of PtO2 under hydrogen (1 atm) at room temperature for 1 h. Filtration and evaporation gave the compound 3 or 4 in quantitative yield. Rf =0.34 (40percent EtOAc in hexane, silica TLC saturated with NH3); IR (CHCl3) ν 3358, 3281, 3013, 2917, 2847, 1595, 1468, 1451, 1437, 747, 718 cm-1; 1

H NMR (CDCl3, 300 MHz) δ 7.35-7.16 (4H, m), 2.94 (1H, dd, J1 =7.1 Hz, J2 =15.5 Hz) 2.65 (1H, dd, J1 =7.7 Hz, J2 =15.5 Hz), 2.21-2.08 (1H, m), 1.94-1.30 (10H, m); C NMR (CDCl3, 125.76 MHz) δ 151.35, 141.67, 126.92, 126.49, 125.46, 121.43, 61.73, 48.72, 35.778, 34.77, 26.42, 22.46, 21.96;

13

MS (70 eV), m/z 187 (M+), 144, 130, 115, 91, 77; HRMS calcd. for C13 H17 N 187.1355, found 187.1355.

3

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80%

Stage #1: piperidine; cyclohexanone With 1H-(1,2,3)triazole in toluene

T=108 - 114°C; Stage #2: Bromure de phenyl magnesium in tetrahydrofuran; toluene

T=24°C; Bruylants reaction; 1.5 h;

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Prashad, Mahavir; Liu, Yugang; Har, Denis; Repic, Oljan; Blacklock, Thomas J.

Tetrahedron Letters, 2005 , vol. 46, # 33 p. 5455 - 5458 Title/Abstract Full Text View citing articles Show Details

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4

Synthesize Find similar Multi-step reaction with 2 steps 1: 50 percent / benzene / 2 h / Heating 2: 73 percent / diethyl ether; benzene / 20 °C View Scheme

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Rx-ID: 20377347 Find similar reactions

Katritzky, Alan R.; Najzarek, Zbigniew; Dega-Szafran, Zofia

Synthesis, 1989 , # 1 p. 66 - 69 Title/Abstract Full Text Show Details

5

Synthesize Find similar Multi-step reaction with 2 steps 1: 50 percent / benzene / 2 h / Heating 2: 73 percent / diethyl ether; benzene / 20 °C View Scheme

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Rx-ID: 20390522 Find similar reactions

Katritzky, Alan R.; Najzarek, Zbigniew; Dega-Szafran, Zofia

Synthesis, 1989 , # 1 p. 66 - 69 Title/Abstract Full Text Show Details

6

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Rx-ID: 28499295 Find similar reactions

58%

Stage #1: bromobenzene With iodine; magnesium in tetrahydrofuran; diethyl ether

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Ahmadi, Abbas; Khalili, Mohsen; Abbassi, Sara; Javadi, Mozhdeh; Mahmoudi, Ali; Hajikhani, Ramin

Arzneimittel-Forschung/Drug Research, 2009 , vol. 59, # 4 p. 202 - 206 Title/Abstract Full Text View citing articles Show Details


Stage #2: 1-piperidin-1-ylcyclohexanecarbonitrile in tetrahydrofuran; diethyl ether

Reflux;

58%

Stage #1: bromobenzene With iodine; magnesium in tetrahydrofuran

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Pakzad, Sara

Asian Journal of Chemistry, 2011 , vol. 23, # 12 p. 5429 - 5432 Title/Abstract Full Text View citing articles Show Details

Stage #2: 1-piperidin-1-ylcyclohexanecarbonitrile in tetrahydrofuran

Stage #1: bromobenzene With iodine; magnesium in tetrahydrofuran

Ahmadi, Abbas; Khalili, Mohsen; Mihandoust, Farnaz; Barghi, Leila

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 1 p. 30 - 35 Title/Abstract Full Text View citing articles Show Details

Stage #2: 1-piperidin-1-ylcyclohexanecarbonitrile

Hide Details Stage #1: bromobenzene With iodine; magnesium in tetrahydrofuran

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Stage #2: 1-piperidin-1-ylcyclohexanecarbonitrile

Stage #1: bromobenzene With iodine; magnesium in diethyl ether Reflux; Stage #2: 1-piperidin-1-ylcyclohexanecarbonitrile in diethyl ether; toluene

Reflux;

Ahmadi; Kermani; Naderi; Hajikhani; Rezaee; Javadi; Niknafs

Current Medicinal Chemistry, 2012 , vol. 19, # 5 p. 763 - 769 Title/Abstract Full Text View citing articles Show Details

7

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Rx-ID: 30653970 Find similar reactions

Multi-step reaction with 2 steps 1: hydrogenchloride 2: iodine; magnesium / tetrahydrofuran View Scheme

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Multi-step reaction with 2 steps 1: hydrogenchloride View Scheme

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Multi-step reaction with 2 steps

Ahmadi; Kermani; Naderi; Hajikhani; Rezaee; Javadi; Niknafs

Current Medicinal Chemistry, 2012 , vol. 19, # 5 p. 763 - 769


1.1: sodium hydrogensulfite 2.1: iodine; magnesium / diethyl ether / Reflux 2.2: Reflux View Scheme

8

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Rx-ID: 30653972 Find similar reactions

58%

9

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Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

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Title/Abstract Full Text View citing articles Show Details

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Rx-ID: 30653974 Find similar reactions

Multi-step reaction with 2 steps 1: hydrogenchloride 2: iodine; magnesium / tetrahydrofuran View Scheme

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Multi-step reaction with 2 steps 1: hydrogenchloride View Scheme

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Multi-step reaction with 2 steps 1.1: sodium hydrogensulfite 2.1: iodine; magnesium / diethyl ether / Reflux 2.2: Reflux View Scheme

Ahmadi; Kermani; Naderi; Hajikhani; Rezaee; Javadi; Niknafs

Current Medicinal Chemistry, 2012 , vol. 19, # 5 p. 763 - 769 Title/Abstract Full Text View citing articles Show Details


10

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Rx-ID: 33447105 Find similar reactions

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Multi-step reaction with 2 steps 1: hydrochlorid acid 2: iodine; magnesium / tetrahydrofuran View Scheme

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Pakzad, Sara

Asian Journal of Chemistry, 2011 , vol. 23, # 12 p. 5429 - 5432 Title/Abstract Full Text View citing articles Show Details

Multi-step reaction with 2 steps 1.1: NaHS03

2.1: iodine / diethyl ether 2.2: |Reflux View Scheme

Ahmadi, Abbas; Khalili, Mohsen; Barzin, Mahnaz; Pooladi, Mohsen; Bakhtiari, Fatemeh; Barjeste, Maede; Nahri-Niknafs, Babak

Monatshefte fur Chemie, 2016 , vol. 147, # 2 p. 457 - 464 Title/Abstract Full Text View citing articles Show Details

11

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Stage #1: bromobenzene; magnesium With iodine in diethyl ether

Bruylants Amination; Stage #2: 1piperidinocyclohexylcarbonitrile in diethyl ether; toluene

Bruylants Amination; Reflux; Hide Experimental Procedure

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Ahmadi, Abbas; Khalili, Mohsen; Barzin, Mahnaz; Pooladi, Mohsen; Bakhtiari, Fatemeh; Barjeste, Maede; Nahri-Niknafs, Babak

Monatshefte fur Chemie, 2016 , vol. 147, # 2 p. 457 - 464 Title/Abstract Full Text View citing articles Show Details

Preparation of compounds 9a–9k

General procedure: A solution of 0.0203 mol nitrile intermediates 1–6 in diethylether and toluene (1:1) were added to phenyl or2-thiophene magnesium bromide reagents (7 and 8, preparedfrom refluxing of 0.0503 mol bromobenzene or2-bromothiophene and 0.505 g of Mg in 100 cm3 of dryether). These mixtures were refluxed for additional hours(monitoring by TLC) and subsequently dipped into thesolution of ice-NH4Cl and NH4OH. The organic layerswere decanted and washed. The bases were acidified with10 percent H2SO4, basified with 10 percent NaOH, neutralized bywashing with water, extracted with ether, dried, and concentrated.The products were obtained as solids or viscousliquid compounds which for purification were passedthrough a silica gel column using ethyl acetate/n-hexane(95:5) as the eluent to yield 9a–9k.


12

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Rx-ID: 6432171 Find similar reactions

Phencyclidin, PdO/T2;

Kalir et al.

Journal of Labelled Compounds and Radiopharmaceuticals, 1977 , vol. 13, p. 445,446,447 Full Text View citing articles Show Details

Tetrahydropyridin 5, Pd/C, T2;

Kalir et al.

Journal of Labelled Compounds and Radiopharmaceuticals, 1977 , vol. 13, p. 445,446,447 Full Text View citing articles Show Details

13

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Rx-ID: 1756823 Find similar reactions

Yield given. Multistep reaction;

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Masumoto; Takeuchi; Ohta; Hirobe

Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 7 p. 1788 - 1794 Title/Abstract Full Text View citing articles Show Details

14

Synthesize Find similar aus Phenyl-d(5)Magnesiumbromid, 1-Piperidinocyclohexancarbonitril;

Rx-ID: 6863288 Find similar reactions

Fentiman; Foltz

Journal of Labelled Compounds and Radiopharmaceuticals, 1976 , vol. 12, p. 69,74 Full Text Show Details


15

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Rx-ID: 38526024 Find similar reactions

Multi-step reaction with 2 steps 1: sodium hydrogensulfite 2: iodine; magnesium / diethyl ether View Scheme

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Ahmadi, Abbas; Khalili, Mohsen; Hajikhani, Ramin; Naserbakht, Moslem

Pharmacology Biochemistry and Behavior, 2011 , vol. 98, # 2 p. 227 - 233 Title/Abstract Full Text View citing articles Show Details

16

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Rx-ID: 38526025 Find similar reactions

Stage #1: bromobenzene With iodine; magnesium in diethyl ether

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Ahmadi, Abbas; Khalili, Mohsen; Hajikhani, Ramin; Naserbakht, Moslem

Pharmacology Biochemistry and Behavior, 2011 , vol. 98, # 2 p. 227 - 233 Title/Abstract Full Text View citing articles Show Details

Stage #2: 1-piperidin-1-ylcyclohexanecarbonitrile in tetrahydrofuran; diethyl ether

Stage #3: With hydrogenchloride in diethyl ether; water; isopropyl alcohol

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1-[1-phenylcyclohexyl] piperidine (PCP) (I)

This compound was prepared in a 58percent yield based on a publishedmethod (Maddox et al., 1965) from adding a solution of 1-piperidinocyclohexanecarbonitrile (1) in an organic solvent to arefluxing solution of phenyl magnesium bromide (prepared from 79 gbromobenzene and 12.3 g of Mg in 200 ml of dry ether). Thehydrochloride salt of I(m.p. 233–234 °C)wasprepared using 2-propanoland HCl, and it was recrystallized from 2propanol.


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