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1571982-04-1

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1571982-04-1 Usage

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.

Check Digit Verification of cas no

The CAS Registry Mumber 1571982-04-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,5,7,1,9,8 and 2 respectively; the second part has 2 digits, 0 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1571982-04:
(9*1)+(8*5)+(7*7)+(6*1)+(5*9)+(4*8)+(3*2)+(2*0)+(1*4)=191
191 % 10 = 1
So 1571982-04-1 is a valid CAS Registry Number.

1571982-04-1Upstream product

1571982-04-1Downstream Products

1571982-04-1Relevant articles and documents

CRYSTAL OF 1,2-DIHYDROPYRIDINE COMPOUND AND METHOD FOR PRODUCING SAME

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Page/Page column 11, (2008/06/13)

The invention provides crystals of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one and production processes therefor.

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