Donepezil Hydrochloride → 2-Pyridin-4-ylmethyl-indan-1-one

HRID 967309

反応式

HRID 967309 の反応式
CO[C:3]1[CH:4]=[C:5]2[CH2:14][CH:13]([CH2:15][CH:16]3[CH2:21][CH2:20][N:19](CC4C=CC=CC=4)[CH2:18][CH2:17]3)[C:11](=[O:12])[C:6]2=[CH:7][C:8]=1OC.Cl.C1(=O)C2C(=CC=CC=2)CC1>>[N:19]1[CH:20]=[CH:21][C:16]([CH2:15][CH:13]2[CH2:14][C:5]3[C:6](=[CH:7][CH:8]=[CH:3][CH:4]=3)[C:11]2=[O:12])=[CH:17][CH:18]=1

参加物

3

反応物 2

HCID 5741Donepezil HydrochlorideHCID 67351-Indanone

生成物 1

HCID 149398002-Pyridin-4-ylmethyl-indan-1-one

実験手順

U.S. Pat. No. 6,252,081 teaches the preparation of Donepezil HCl by the reaction of 1-indanone derivative with carbonate ester. The resulting 2-alkoxycarbonyl-1-indanone derivative is halogenated with (4-pyridyl) methyl or a salt thereof and decarboxylated successively to give 2-(4-pyridyl)methyl-1-indanone derivative. On reacting the 2-(4-pyridyl) methyl-1-indanone derivative with benzyl bromide, their quaternary ammonium salts are formed, which on reduction with platinum oxide catalyst gives Donepezil HCl (Examples 1 to 3). Overall yield of Donepezil HCl 82% (98%×85%×100%×99%).

出典と根拠

ORDレコード
ord-b95b91bd195c4f3eb1a89704e873dbec
出典データセット
uspto-grants-2005_10
特許番号
US06953856B2

関連ノート

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