perampanel 3/4 hydrate

perampanel 3/4 hydrate 구조식 이미지
카스 번호:
1571982-04-1
상품명:
perampanel 3/4 hydrate
동의어(영문):
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
분자식:
C23H17N3O2
포뮬러 무게:
367.41
MOL 파일:
1571982-04-1.mol

perampanel 3/4 hydrate 속성

안전

perampanel 3/4 hydrate C화학적 특성, 용도, 생산

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.

Synthesis_1571982-04-1

perampanel 3/4 hydrate 준비 용품 및 원자재

원자재

준비 용품


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