perampanel 3/4 hydrate
- Product Name
- perampanel 3/4 hydrate
- CAS No.
- 1571982-04-1
- Chemical Name
- perampanel 3/4 hydrate
- Synonyms
- Perampanel Hydrate;4 hydrate;perampanel 3;Perampanel 3/4H2O;perampanel 3/4 hydrate;Perampanel hydrate (4:3);3-(2-CYANOPHENYL)-1-PHENYL-5-(2-PYRIDYL)-1,2-DIHYDROPYRIDIN-2-ONE 3/4 HYDRATE;2-(1',6'-Dihydro-6'-oxo-1'-phenyl[2,3'-bipyridin]-5'-yl)benzonitrile hydrate (4:3)
- CBNumber
- CB03059139
- Molecular Formula
- C23H17N3O2
- Formula Weight
- 367.41
- MOL File
- 1571982-04-1.mol
perampanel 3/4 hydrate Chemical Properties,Usage,Production
Definition
ChEBI: Perampanel hydrate is a hydrate obtained by combining four molecules of perampanel with three molecules of water. Used as an adjunctive therapy for the treatment of partial-onset seizures in patients with epilepsy. It has a role as an AMPA receptor antagonist and an anticonvulsant. It contains a perampanel.
Clinical Use
Perampanel is a selective, non-competitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) antagonist approved for partial-onset seizures in patients with epilepsy. Perampanel was discovered and developed by Eisai.
Synthesis
A number of synthetic routes to perampanel have been reported and the process scale route is described herein.Bromination of commercial 2-methoxypyridine (120) gave 5-bromo-2-methoxypridine 121 in 86% yield (the scheme). Lithium halogen exchange was then accomplished by treating 121 with nbutyllithium followed by reaction with 2-benzenesulfonylpyridine (122) to provide bi-aryl 123 which was hydrolyzed under acidic conditions to give pyridine 124 in 60% overall yield. N-Arylation with triphenylboroxine (125) in the presence of copper acetate afforded N-aryl pyridine 126 in 91% yield. Pyridone 126 was reacted with N-bromosuccinimide to give bromopyridine 127 which was coupled with 2-(1,3,2-dioxaborinan-2-yl)benzonitrile (128) under palladium catalyzed conditions to give perampanel hydrate (XIX) in 86% yield after recrystallization from acetone/H2O.
perampanel 3/4 hydrate Preparation Products And Raw materials
Raw materials
Preparation Products
perampanel 3/4 hydrate Suppliers
- Tel
- 86-(0)29-85992781 17792393971
- info@lynnchem.com
- Country
- China
- ProdList
- 4587
- Advantage
- 58
- Tel
- 15374522761
- Fax
- QQ:2853117752
- 3003392093@qq.com
- Country
- China
- ProdList
- 8789
- Advantage
- 55
- Tel
- 021-50630626 15821189163
- sales@witofly.com
- Country
- China
- ProdList
- 1605
- Advantage
- 55
- Tel
- 44-20819178-90 02081917890
- Fax
- (0)2080432064
- info@novachemistry.com
- Country
- United Kingdom
- ProdList
- 4381
- Advantage
- 58
- Tel
- +8618229978283 19294230172
- sales@chemfish.com
- Country
- China
- ProdList
- 4888
- Advantage
- 58
- Tel
- +86-571-86088112
- info@proserre.com
- Country
- China
- ProdList
- 1077
- Advantage
- 58
- Tel
- +86-0731-85567275 18932438858
- Fax
- QQ:3554193828
- sales05@chemfish.com
- Country
- China
- ProdList
- 8355
- Advantage
- 58
- Tel
- 021-021-50630626 18964684208
- Fax
- 021-50563898
- kate@tajilin.com
- Country
- China
- ProdList
- 1265
- Advantage
- 58
- Tel
- 021-51816796-820 13611835272
- Fax
- 021-5161 3951
- sales2@sunwaypharm.com
- Country
- China
- ProdList
- 44455
- Advantage
- 58
- Tel
- 15623309010
- 1287744812@qq.com
- Country
- China
- ProdList
- 1678
- Advantage
- 58