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18162-48-6872-50-4Methylene ChloridenaphthaleneTHFTitanium Dioxide
ChemicalBook CAS DataBase List PeraMpanel

PeraMpanel synthesis

5synthesis methods
Perampanel is discontinued (DEA controlled substance). Perampanel is a selective noncompetitive antagonist of AMPA receptors, the major subtype of ionotropic glutamate receptors. Perampanel was found to be effective in the treatment of refractory partial-onset seizures in clinical trials.
Synthetic Routes
  • ROUTE 1

    • 202112078677731140.jpg

    : Hibi, Shigeki; Ueno, Koshi; Nagato, Satoshi; Kawano, Koki; Ito, Koichi; Norimine, Yoshihiko; Takenaka, Osamu; Hanada, Takahisa; Yonaga, Masahiro. Discovery of 2-​(2-​Oxo-​1-​phenyl-​5-​pyridin-​2-​yl-​1,​2-​dihydropyridin-​3-​yl)​benzonitrile (Perampanel)​: A Novel, Noncompetitive α-​Amino-​3-​hydroxy-​5-​methyl-​4-​isoxazolepropanoic Acid (AMPA) Receptor Antagonist. Journal of Medicinal Chemistry. Volume 55. Issue 23. Pages 10584-10600. Journal; Online Computer File. (2012).

  • ROUTE 2

    • 202112073124343244.jpg

    McElhinny, Charles J., Jr.; Carroll, F. I.; Lewin, Anita H. A practical, laboratory-​scale synthesis of perampanel. Synthesis. Volume 44. Issue 1. Pages 57-62. Journal. (2012).

  • ROUTE 3

    • 202112079645415612.jpg

    Lee, Hong Geun; Milner, Phillip J.; Placzek, Michael S.; Buchwald, Stephen L.; Hooker, Jacob M. Virtually Instantaneous, Room-​Temperature [11C]​-​Cyanation Using Biaryl Phosphine Pd(0) Complexes. Journal of the American Chemical Society. Volume 137. Issue 2. Pages 648-651. Journal; Online Computer File. (2015).

  • ROUTE 4

    • 202112071320572933.jpg

    Dahanukar, Vilas Hareshwar; Iqbal, Javed; Oruganti, Srinivas; Rapolu, Rajesh Kumar. Preparation of perampanel. Assignee Dr. Reddys Laboratories Limited, India. IN 2013CH02042. (2016).

  • ROUTE 5

    • 202112079183270477.jpg

    Kapkoti, Gobind Singh; Lourdusamy, Mettilda; Radu, Ioan Iosif; Pandya, Ashesh Kamalnayan; Chauhan, Nitesh Dolatram; Dholariya, Bipinkumar Hashmukhbhai; Patel, Vishal Keshavlal. Novel process for the preparation of perampanel and its intermediates thereof. Assignee Intas Pharmaceuticals Ltd., India. WO 2016147104. (2016).

  • ROUTE 6

    • 202112074119249704.jpg

    : Marom, Ehud; Rubnov, Shai. Process and intermediates for the preparation of perampanel. Assignee Mapi Pharma Ltd., Israel. WO 2016132343. (2016).

  • ROUTE 7

    • 202112075337619292.jpg

    Desai, Sanjay Jagdish; Parihar, Jayprakash Ajitsingh; Jain, Kuldeep Natwarlal; Patil, Sachin Ashokrao. Process for the preparation of perampanel. Assignee Cadila Healthcare Limited, India. US 20160039759. (2016).

  • ROUTE 8

    • 202112077758230292.jpg

    Buchlovic, Marian. Process for the preparation of perampanel. Assignee Ivax International GmbH, Switz.; Teva Pharmaceuticals USA, Inc. WO 2015013520. (2015).

  • ROUTE 9

    • 202112079277821518.jpg

    Ye, Tianjian; Yu, Guangliang; Ma, Suwang. A process for preparing perampanel and its intermediates. Assignee Zhejiang Yongning Pharmaceutical Co., Ltd., Peop. Rep. China. CN 103980188. (2014).

  • ROUTE 10

    • 202112070520980235.jpg

    Arimoto, Itaru; Nagato, Satoshi; Sugaya, Yukiko; Urawa, Yoshio; Ito, Koichi; Naka, Hiroyuki; Omae, Takao; Kayano, Akio; Nishiura, Katsutoshi. Process for preparation of 1,2-dihydropyridine-2-one derivatives. Assignee Eisai R&D Management Co., Ltd., Japan. US 20070142640. (2007).

202112078677731140.jpg

: Hibi, Shigeki; Ueno, Koshi; Nagato, Satoshi; Kawano, Koki; Ito, Koichi; Norimine, Yoshihiko; Takenaka, Osamu; Hanada, Takahisa; Yonaga, Masahiro. Discovery of 2-​(2-​Oxo-​1-​phenyl-​5-​pyridin-​2-​yl-​1,​2-​dihydropyridin-​3-​yl)​benzonitrile (Perampanel)​: A Novel, Noncompetitive α-​Amino-​3-​hydroxy-​5-​methyl-​4-​isoxazolepropanoic Acid (AMPA) Receptor Antagonist. Journal of Medicinal Chemistry. Volume 55. Issue 23. Pages 10584-10600. Journal; Online Computer File. (2012).

381248-06-2 Synthesis
5'-broMo-1'-phenyl-[2,3'-bipyridin]-6'(1'H)-one

381248-06-2
86 suppliers
$34.00/100mg

2-(1,3,2-DIOXABOROLAN-2-YL)BENZONITRILE

172732-52-4
242 suppliers
$19.00/1g

PeraMpanel

380917-97-5
142 suppliers
$79.00/5mg

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Yield:380917-97-5 73%

Reaction Conditions:

with caesium carbonate;palladium dichloride in N,N-dimethyl-formamide at 80; for 6 h;Inert atmosphere;Suzuki-Miyaura Coupling;

References:

Hibi, Shigeki;Ueno, Koshi;Nagato, Satoshi;Kawano, Koki;Ito, Koichi;Norimine, Yoshihiko;Takenaka, Osamu;Hanada, Takahisa;Yonaga, Masahiro [Journal of Medicinal Chemistry,2012,vol. 55,# 23,p. 10584 - 10600]

380917-96-4

380917-96-4
2 suppliers
inquiry

98-80-6 Synthesis
Phenylboronic acid

98-80-6
697 suppliers
$5.00/5g

PeraMpanel

380917-97-5
142 suppliers
$79.00/5mg

References
Benzonitrile, 2-(1',6'-dihydro-6'-oxo-1'-phenyl[2,3'-bipyridin]-5'-yl)-, hydrate (1:1)

942063-28-7
0 suppliers
inquiry

PeraMpanel

380917-97-5
142 suppliers
$79.00/5mg

References
381233-78-9 Synthesis
5-(2-PYRIDYL)-1,2-DIHYDROPYRIDIN-2-ONE

381233-78-9
165 suppliers
$9.00/100mg

PeraMpanel

380917-97-5
142 suppliers
$79.00/5mg

References
3,5-DIBROMO-2-HYDROXYPYRIDINE

13472-81-6
199 suppliers
$9.00/1g

PeraMpanel

380917-97-5
142 suppliers
$79.00/5mg

References

PeraMpanel Related Search:

Levetiracetam Unii-4bmh7izt98 Entacapone 3,5-Dibromopyridine PeraMpanel PeraMpanel Phenylboronic acid 3,5-Dimethoxypyridine 2-(2-cyanophenyl)benzonitrile 5-(2-PYRIDYL)-1,2-DIHYDROPYRIDIN-2-ONE