4-Piperidineethanol → 2-[1-(6-Fluoro-1-isoquinolyl)-4-piperidyl]ethanol

反応式

Cl[C:2]1[C:11]2[C:6](=[CH:7][C:8]([F:12])=[CH:9][CH:10]=2)[CH:5]=[CH:4][N:3]=1.[NH:13]1[CH2:18][CH2:17][CH:16]([CH2:19][CH2:20][OH:21])[CH2:15][CH2:14]1>>[F:12][C:8]1[CH:7]=[C:6]2[C:11](=[CH:10][CH:9]=1)[C:2]([N:13]1[CH2:18][CH2:17][CH:16]([CH2:19][CH2:20][OH:21])[CH2:15][CH2:14]1)=[N:3][CH:4]=[CH:5]2

参加物

反応物 2

HCID 739534-Piperidineethanol

HCID 219010721-Chloro-6-fluoroisoquinoline

生成物 1

HCID 210969282-[1-(6-Fluoro-1-isoquinolyl)-4-piperidyl]ethanol収率 39.1%

実験手順

The process is performed as described in Example 4 (step 4.1). Starting with 1.52 g (8.39 mmol) of 1-chloro-6-fluoroisoquinoline and 1.20 g (9.23 mmol) of 2-(4-piperidyl)ethanol, and after chromatography on silica gel, eluting with a 95/5/0.5 mixture of dichloromethane, methanol and 28% aqueous ammonia, 0.90 g of pure product is obtained in the form of a yellow paste.

後処理

washafter chromatography on silica gel, eluting with a 95/5/0.5 mixture of dichloromethane, methanol and 28% aqueous ammonia

出典と根拠

ORDレコード: ord-2051e1eff46743c4af85a18f7ebb911f
出典データセット: uspto-grants-2007_05
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US07214798B2

反応ノート

読み込み中…

参加物