1-(4-Fluorophenyl)-2-methylpropan-2-amine [C10H14FN]

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Date

3 substances in Reaxys

2018-06-09 08h:23m:26s (UTC)

H 2N

1. Query F

Search as: As drawn ))

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Reaxys ID 20586848 View in Reaxys

1/3 Linear Structure Formula: C10H14 (18)FN Molecular Formula: C10H14FN Molecular Weight: 166.228 InChI Key: JITFIYFVPMQJOK-KXMUYVCJSA-N Note:

18F

H 2N

Patent-Specific Data (1) Prophetic ComLocation in Patent pound prophetic product

Page/page column 150

References Patent; PRESIDENT AND FELLOWS OF HARVARD COLLEGE; RITTER, Tobias; BRASS, Laura; KEITH, Curtis; WATSON, Alan; GREENBLATT, David, J.; WO2010/81036; (2010); (A2) English, View in Reaxys

Druglikeness (1) 1 of 1

LogP

2.34

H Bond Donors

1

H Bond Acceptors

1

Rotatable Bonds

2

TPSA

26.02

Lipinski Number

4

Veber Number

2

Reaxys ID 2802368 View in Reaxys

2/3 CAS Registry Number: 1200-27-7 Chemical Name: 1-(4-fluorophenyl)-2-methylpropan-2-amine; 2-(4fluorophenyl)-1,1-dimethylethylamine; 1-(4-fluorophenyl)-2-methylpropan -2-amine; 1,1-dimethyl-2-(p-fluorophenyl)ethylamine; 1-(4fluorophenyl)-2-methyl-2-propylamine; 2-(4-fluorophenyl)1,1-dimethylethylamine; 4-fluoro-α,α-dimethylphenethylamine Linear Structure Formula: C10H14FN Molecular Formula: C10H14FN Molecular Weight: 167.226 Type of Substance: isocyclic InChI Key: JITFIYFVPMQJOK-UHFFFAOYSA-N Note:

H 2N

F

Substance Label (4) Label References 8-4

Guo, Taijie; Meng, Genyi; Zhan, Xiongjie; Yang, Qian; Ma, Tiancheng; Xu, Long; Sharpless, K. Barry; Dong, Jiajia; Angewandte Chemie - International Edition; vol. 57; nb. 10; (2018); p. 2605 - 2610; Angew. Chem.; vol. 130; nb. 10; (2018); p. 2635 - 2640,6, View in Reaxys

155

Patent; Chinese Academy Of Sciences Shanghai Organic Chemistry Institute; Dong Jiajia; Yang Qian; Guo Taijie; Zhan Xiongjie; Meng Genyi; (59 pag.); CN107857730; (2018); (A) Chinese, View in Reaxys

XIVa

Patent; WYETH; WO2007/143014; (2007); (A2) English, View in Reaxys

Table 2, Amine 1

Kawahata, Noriyuki H.; Brookes, Jeseca; Makara, Gergely M.; Tetrahedron Letters; vol. 43; nb. 40; (2002); p. 7221 - 7223, View in Reaxys

Patent-Specific Data (4) Prophetic ComLocation in Patent pound

References Patent; Pathway Therapeutics Inc.; US2012/252802; (2012); (A1) English, View in Reaxys

prophetic product

Page/page column 150

Patent; PRESIDENT AND FELLOWS OF HARVARD COLLEGE; RITTER, Tobias; BRASS, Laura; KEITH, Curtis; WATSON, Alan; GREENBLATT, David, J.; WO2010/81036; (2010); (A2) English, View in Reaxys Patent; Eisai RandD Management Co., Ltd.; EP2019093; (2009); (A1) English, View in Reaxys

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Patent; ASTRAZENECA AB; WO2008/136756; (2008); (A1) English, View in Reaxys Druglikeness (1) 1 of 1

LogP

2.34

H Bond Donors

1

H Bond Acceptors

1

Rotatable Bonds

2

TPSA

26.02

Lipinski Number

4

Veber Number

2

Derivative (7) Comment (Derivative)

References

Hydrochlorid:F: 181-186grad

Patent; Tropon; GB1037027; (1966); Chem.Abstr.; vol. 65; nb. 12136h; (1966), View in Reaxys

Hydrochlorid: F: 185-186grad

Patent; Troponwerke Dinklage; NL6503967; (1966); Chem.Abstr.; vol. 66; nb. 55205, View in Reaxys

HCl. F:185-186grad

Patent; Troponwerke Dinklage andCo.; FRM4578; (1965); Chem.Abstr.; vol. 69; nb. 86593e; (1968), View in Reaxys

*HCl: F: 185-186grad

Patent; Troponwerke Dinklage; DE1199779; (1965); Chem.Abstr.; vol. 63; nb. 17967a; (1965), View in Reaxys

HCl: F: 185-186grad

Patent; Troponwerke Dinklage; FRCAM66; (1963); Chem.Abstr.; vol. 62; nb. 13087g; (1965), View in Reaxys

HCl-Salz: F: 185-186grad

Patent; Troponwerke Dinklage u. Co.; BE636858; (1963); Chem.Abstr.; vol. 62; nb. 3976d; (1965), View in Reaxys

Hydrochlorid: F: 187grad

Patent; Science Union et Cie-Soc. Francaise de Recherches Medicales; BE609630; (1960); Chem.Abstr.; vol. 60; nb. 1647b; (1964), View in Reaxys

Melting Point (1) 1 of 1

Melting Point [°C]

98

Patent; Societe Wagentaise; FRM4288; (1964); Chem.Abstr.; vol. 68; nb. 59250p; (1968), View in Reaxys Boiling Point (3) Boiling Point [°C] 67

Pressure (Boiling Point) [Torr]

References

4

Patent; Troponwerke Dinklage; DE1199779; (1965); Chem.Abstr.; vol. 63; nb. 17967a; (1965), View in Reaxys; Patent; Tropon; GB1037027; (1966); Chem.Abstr.; vol. 65; nb. 12136h; (1966), View in Reaxys; Patent; Troponwerke Dinklage; NL6503967; (1966); Chem.Abstr.; vol. 66; nb. 55205, View in Reaxys; Patent; Troponwerke Dinklage; FRCAM66; (1963); Chem.Abstr.; vol. 62; nb. 13087g; (1965), View in Reaxys

67 82 - 83

Patent; Troponwerke Dinklage andCo.; FRM4578; (1965); Chem.Abstr.; vol. 69; nb. 86593e; (1968), View in Reaxys 9

Patent; Science Union et Cie-Soc. Francaise de Recherches Medicales; BE609630; (1960); Chem.Abstr.; vol. 60; nb. 1647b; (1964), View in Reaxys

Refractive Index (2) Refractive Index Wavelength (ReTemperature (Refractive Index) [nm] fractive Index) [°C] 1.4942

589

1.4942

589

20.5

References Patent; Troponwerke Dinklage; DE1199779; (1965); Chem.Abstr.; vol. 63; nb. 17967a; (1965), View in Reaxys; Patent; Troponwerke Dinklage; NL6503967; (1966); Chem.Abstr.; vol. 66; nb. 55205, View in Reaxys; Patent; Troponwerke Dinklage andCo.; FRM4578; (1965); Chem.Abstr.; vol. 69; nb. 86593e; (1968), View in Reaxys; Patent; Troponwerke Dinklage; FRCAM66; (1963); Chem.Abstr.; vol. 62; nb. 13087g; (1965), View in Reaxys Patent; Tropon; GB1037027; (1966); Chem.Abstr.; vol. 65; nb. 12136h; (1966), View in Reaxys

Further Information (1)

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Description (Further Information)

References

Further information Patent; Troponwerke Dinklage u. Co.; BE636858; (1963); Chem.Abstr.; vol. 62; nb. 3976d; (1965), View in Reaxys Medchem (6) 1 of 6

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antimicrobial activity of the compound was determined in mice; + = Test performed

Biological Species/NCBI ID

mouse

Substance RN

2802368View in Reaxys

Measurement Parameter

Activity

Qualitative value

ND

Bergmann; Goldschmidt; Journal of medicinal chemistry; vol. 11; nb. 6; (1968); p. 1242 - 1244, View in Reaxys 2 of 6

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anesthetic activity of the compound was determined in rabbit; + = Test performed

Biological Species/NCBI ID

Leporidae

Substance RN

2802368View in Reaxys

Measurement Parameter

Activity

Qualitative value

ND

Bergmann; Goldschmidt; Journal of medicinal chemistry; vol. 11; nb. 6; (1968); p. 1242 - 1244, View in Reaxys 3 of 6

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

General CNS activity in mouse was determined; + = Test performed

Biological Species/NCBI ID

mouse

Substance RN

2802368View in Reaxys

Measurement Parameter

Activity

Measurement Object

CNS activity in mouse

Qualitative value

ND

Bergmann; Goldschmidt; Journal of medicinal chemistry; vol. 11; nb. 6; (1968); p. 1242 - 1244, View in Reaxys 4 of 6

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Minimal effective dose of the compound causing CNS stimulation when administered orally in mice

Biological Species/NCBI ID

mouse

Substance RN

2802368View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

MED

Unit

mg/kg

Measurement Object

Minimal effective dose

Qualitative value

=

Quantitative value

15

Bergmann; Goldschmidt; Journal of medicinal chemistry; vol. 11; nb. 6; (1968); p. 1242 - 1244, View in Reaxys 5 of 6

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Analgesic activity of the compound was determined in mice; + = Test performed

Biological Species/NCBI ID

mouse

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Substance RN

2802368View in Reaxys

Measurement Parameter

Activity

Qualitative value

ND

Bergmann; Goldschmidt; Journal of medicinal chemistry; vol. 11; nb. 6; (1968); p. 1242 - 1244, View in Reaxys 6 of 6

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Anorexic activity of the compound was determined in mice; - = Not tested for activity indicated

Biological Species/NCBI ID

mouse

Substance RN

2802368View in Reaxys

Qualitative Results

-

Measurement Parameter

Activity

Measurement Object

anorexic activity

Qualitative value

NA

Measurement pX

1

Bergmann; Goldschmidt; Journal of medicinal chemistry; vol. 11; nb. 6; (1968); p. 1242 - 1244, View in Reaxys

Reaxys ID 14932033 View in Reaxys

3/3 CAS Registry Number: 2413-54-9 Chemical Name: 2-(4-fluoro-phenyl)-1,1-dimethyl-ethylamine hydrochloride; 2-(4-fluorophenyl)- 1,1-dimethylethylamine hydrochloride; 2-(4-fluorophenyl)-1,1-dimethylethylamine hydrochloride; Dimethyl-4-fluorobenzylmethanamine.hydrochloride Linear Structure Formula: C10H14FN*ClH Molecular Formula: C10H14FN*ClH Molecular Weight: 203.687 InChI Key: WXNVDQWUGUEUMO-UHFFFAOYSA-N Note:

H 2N H

Cl

F

Druglikeness (1) 1 of 1

LogP

2.852

H Bond Donors

1

H Bond Acceptors

1

Rotatable Bonds

2

TPSA

26.02

Lipinski Number

4

Veber Number

2

Melting Point (1) 1 of 1

Patent; Merrell Pharmaceuticals Inc.; US5532397; (1996); (A) English, View in Reaxys

NMR Spectroscopy (1) 1 of 1

Nucleus (NMR Spectroscopy)

1H

Solvents (NMR Spectroscopy)

dimethylsulfoxide-d6; water-d2

Frequency (NMR Spectro- 300 scopy) [MHz] Original Text (NMR Spec- 1H NMR: (DMSO-</6, with 2 drops D2O, 300 MHz): α 7.31 - 7.16 (m, 4H), 2.86 (s, 2 H), 1.20 (s, troscopy) 6H)

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Comment (NMR Spectroscopy)

Signals given

Patent; WYETH; WO2007/143014; (2007); (A2) English, View in Reaxys

Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.

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